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176 results about "Azepine" patented technology

Azepines are unsaturated heterocycles of seven atoms, with a nitrogen replacing a carbon at one position.

Azepine inhibitors of Janus kinases

InactiveUS20070149506A1BiocideSenses disorderMedicineJanus kinase
Azepine inhibitors of Janus kinases
Azepine inhibitors of Janus kinases
Azepine inhibitors of Janus kinases
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Owner:INCYTE

Azepine inhibitors of janus kinases

InactiveUS20090197869A1BiocideSenses disorderJanus kinase activityMedicine
Azepine inhibitors of janus kinases
Azepine inhibitors of janus kinases
Azepine inhibitors of janus kinases
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Owner:INCYTE CORP

Azepine argireline or pharmaceutically acceptable salt thereof and preparation method and application thereof

ActiveCN101648994AHigh purityShort routeAntimycoticsPeptide preparation methodsPeptideAzepine
Azepine argireline or pharmaceutically acceptable salt thereof and preparation method and application thereof
Azepine argireline or pharmaceutically acceptable salt thereof and preparation method and application thereof
Azepine argireline or pharmaceutically acceptable salt thereof and preparation method and application thereof
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Owner:SHANGHAI TECHWELL BIOPHARMACEUTICALS CO LTD

Process for preparing hexahydropyrimido[1,2-a]azepine-2-carboxylates and related compounds

InactiveUS20070142635A1High yieldLow costAntiviralsPhosphorus organic compoundsCarboxylic saltHIV Integrase Inhibitors
Processes for preparing 10-amino-3-hydroxy-4-oxo-4,6,7,8,9,10-hexahydropyrimido[1,2-a]azepine-2-carboxylates and related compounds are disclosed. The preparation of carboxamide derivatives from these carboxylates is also disclosed. The carboxamides are HIV integrase inhibitors and are useful for treating HIV infection and AIDS.
Process for preparing hexahydropyrimido[1,2-a]azepine-2-carboxylates and related compounds
Process for preparing hexahydropyrimido[1,2-a]azepine-2-carboxylates and related compounds
Process for preparing hexahydropyrimido[1,2-a]azepine-2-carboxylates and related compounds
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Owner:ASKIN DAVID +5

Fused azepine derivatives and their use as antidiuretic agents

InactiveUS20040038962A1BiocideNervous disorderAgonistAVP - Arginine vasopressin
Fused azepine derivatives and their use as antidiuretic agents
Fused azepine derivatives and their use as antidiuretic agents
Fused azepine derivatives and their use as antidiuretic agents
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Owner:VANTIA

Aliphatic-aromatic copolyester, preparation method and application thereof

ActiveCN101717493AAvoid problems such as affecting performanceEvenly dispersedAdhesivesCarboxylic acid halidesMonomer
The invention provides aliphatic-aromatic copolyester, a preparation method and application thereof. Polymerization monomers comprise a compound selected from aliphatic dibasic acid, and naphthenic base dibasic acid or the ester, the anhydride and the acyl halide thereof, a compound selected from aromatic dibasic acid or the ester, the anhydride and the acyl halide thereof, a compound simultaneously with two functional groups selected from an amino-group, a mercapto group or a hydroxy or a compound of a derivative of the amino-group, the mercapto group or the hydroxyl with an epoxy group and an azepine ring, a compound selected from unsaturated acid with at least one C-C, C-O, C-N or C-S double bond and C-C or C-N triple bond or the ester, the anhydride and the acyl halide thereof and a compound of unsaturated alcohol with at least one C-C double bond or a C-C triple bond or an epoxide thereof. The aliphatic-aromatic copolyester is prepared by carrying out esterification and polycondensation after mixing the polymerization monomers, polymerizing the double bonds and/or the triple bonds on the polymerization monomers under the action of an initiator and then carrying out a graftingand/or coupling reaction.
Aliphatic-aromatic copolyester, preparation method and application thereof
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Owner:HANGZHOU XINFU TECH CO LTD

Condensed azepines as vasopressin agonists

InactiveUS20030087892A1BiocideOrganic chemistryAgonistAntidiuretic
This invention provides novel compounds according to general formula (1) wherein A is a bicyclic or tricyclic azepine derivative, V1 and V2 are both H, OMe or F, or one of V1 and V2 is Br, Cl, F, OH, OMe, OBn, OPh, O-acyl, N3, NH2, NHBn or NH-acyl and the other is H, or V1 and V2 together are =O, -O(CH2)pO- or -S(CH2)pS-; W1 is either O or S; X1 and X2 are both H, or together are =O or =S; Y is OR5 or NR6R7; R1, R2, R3 and R4 are independently selected from H, lower alkyl, lower alkyloxy, F, Cl and Br; R5 is selected from H and lower alkyl; R6 and R7 are independently selected from H and lower alkyl, or together are -(CH2)n; n=3, 4, 5, 6; and p is 2 or 3. The compounds are agonists at the vasopressin V2 receptor and are useful as antidiuretics and procoagulants. The invention further comprises pharmaceutical compositions incorporating these vasopressin agonists, which compositions are particularly useful in the treatment of central diabetes insipidus, nocturnal enuresis and nocturia.
Condensed azepines as vasopressin agonists
Condensed azepines as vasopressin agonists
Condensed azepines as vasopressin agonists
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Owner:VANTIA

Condensed azepines as vasopressin agonists

InactiveUS7074781B2BiocideOrganic chemistryAgonistAntidiuretic
This invention provides novel compounds according to general formula (1) wherein A is a bicyclic or tricyclic azepine derivative, V1 and V2 are both H, OMe or F, or one of V1 and V2 is Br, Cl, F, OH, OMe, OBn, OPh, O-acyl, N3, NH2, NHBn or NH-acyl and the other is H, or V1 and V2 together are ═O, —O(CH2)pO— or —S(CH2)pS—; W1 is either O or S; X1 and X2 are both H, or together are ═O or ═S; Y is OR5 or NR6R7; R1, R2, R3 and R4 are independently selected from H, lower alkyl, lower alkyloxy, F, Cl and Br; R5 is selected from H and lower alkyl; R6 and R7 are independently selected from H and lower alkyl, or together are —(CH2)n—; n=3, 4, 5, 6; and p is 2 or 3. The compounds are agonists at the vasopressin V2 receptor and are useful as antidiuretics and procoagulants. The invention further comprises pharmaceutical compositions incorporating these vasopressin agonists, which compositions are particularly useful in the treatment of central diabetes insipidus, nocturnal enuresis and nocturia.
Condensed azepines as vasopressin agonists
Condensed azepines as vasopressin agonists
Condensed azepines as vasopressin agonists
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Owner:VANTIA

5,6-dihydro-4H-benzo[b]thieno-[2,3-d]azepine derivative

ActiveUS9732098B2Powder deliveryOrganic chemistryDiseaseBenzothiophene
5,6-dihydro-4H-benzo[b]thieno-[2,3-d]azepine derivative
5,6-dihydro-4H-benzo[b]thieno-[2,3-d]azepine derivative
5,6-dihydro-4H-benzo[b]thieno-[2,3-d]azepine derivative
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Owner:PULMOCIDE

AZINONE-SUBSTITUTED AZEPINO[b]INDOLE AND PYRIDO-PYRROLO-AZEPINE MCH-1 ANTAGONISTS, METHODS OF MAKING, AND USE THEREOF

ActiveUS20110003793A1High affinityHigh indexBiocideNervous disorderDiseaseMedicine
AZINONE-SUBSTITUTED AZEPINO[b]INDOLE AND PYRIDO-PYRROLO-AZEPINE MCH-1 ANTAGONISTS, METHODS OF MAKING, AND USE THEREOF
AZINONE-SUBSTITUTED AZEPINO[b]INDOLE AND PYRIDO-PYRROLO-AZEPINE MCH-1 ANTAGONISTS, METHODS OF MAKING, AND USE THEREOF
AZINONE-SUBSTITUTED AZEPINO[b]INDOLE AND PYRIDO-PYRROLO-AZEPINE MCH-1 ANTAGONISTS, METHODS OF MAKING, AND USE THEREOF
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Owner:HARMONY BIOSCIENCES LLC +1

Citric acid tropisetron raw material medicine and preparation technology of raw material medicine and injection liquid

ActiveCN101838266AGood curative effectImprove securityOrganic chemistryDigestive systemTropaneFormate
The invention relates to a citric acid tropisetron raw material medicine and a preparation technology of the citric acid tropisetron raw material medicine and an injection liquid, and belongs to the field of chemical pharmacy; in the process of tropisetron salifying, the citric acid is used as acid radical; the chemical name of the citric acid tropane tropisetron is [(1alpha H, 5alpha H)-8-methyl-azepine bicyclo-(3, 2, 1) octyl group-3alpha-]-1H- benzpyrole-3- formic ether citrate; and the molecular formula is C23H28N209. In the process of tropisetron salifying, the tropisetron is dissolved in ethanol; the mixture is added with ethanol solution of the citric acid, evenly stirred and stands till the needed solid is separated out; the crude citric acid tropisetron is filtered, heated and dissolved in distilled water, is added with the activated carbon for backflowing and decoloring, cools and stands after being filtered so as to separate out white cystal; the mixture is filtered; the filter cake is dried and then distilled water is used for the secondary recrystallization to obtain the refined citric acid tropane tropisetron. The clinical research shows that compared with the imported muriatic acid tropisetron injection solution, the citric acid tropisetron injection solution has similar curative effect and safety.
Citric acid tropisetron raw material medicine and preparation technology of raw material medicine and injection liquid
Citric acid tropisetron raw material medicine and preparation technology of raw material medicine and injection liquid
Citric acid tropisetron raw material medicine and preparation technology of raw material medicine and injection liquid
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Owner:JIANGXI DONGFU PHARMA CO LTD

Substituted hexahydropyrrolo[1,2-a]pyrazines, octahydropyrido[1,2-a]-pyrazines and decahydropyrazino[1,2-a]azepines

InactiveUS6906060B2BiocideOrganic chemistryDiseaseHistamine H1 receptor
Substituted hexahydropyrrolo[1,2-a]pyrazines, octahydropyrido[1,2-a]-pyrazines and decahydropyrazino[1,2-a]azepines
Substituted hexahydropyrrolo[1,2-a]pyrazines, octahydropyrido[1,2-a]-pyrazines and decahydropyrazino[1,2-a]azepines
Substituted hexahydropyrrolo[1,2-a]pyrazines, octahydropyrido[1,2-a]-pyrazines and decahydropyrazino[1,2-a]azepines
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Owner:VTV THERAPEUTICS LLC

Synthesis method of epinastine

ActiveCN103012408ASynthetic Method AdvantagesReduce usageOrganic chemistrySilanesSynthesis methods
The invention discloses a synthesis method of epinastine. The synthesis method is implemented by taking 2-aminobenzophenone as a raw material and comprises the following steps of: reacting the 2-aminobenzophenone with a silane agent to obtain 2-benzylaniline; then, carrying out acylation reaction on the 2-benzylaniline and 2-chloroacetyl chloride to obtain N-(2-benzyl phenyl)-2-chloroacetamide; carrying out acidamide dehydration and cyclization on the N-(2-benzyl phenyl)-2-chloroacetamide under the action of a dehydrating agent to obtain 6-(chloromethyl)-11H-dibenzo[b,e] azepine; carrying out azidation reaction on the 6-(chloromethyl)-11H-dibenzo[b,e] azepine to obtain 6-(azido-methytbiphenyl)-11H-dibenzo[b,e] azepine; carrying out reduction on the 6-(azido-methytbiphenyl)-11H-dibenzo[b,e] azepine to obtain 6-(aminomethyl)-6,11-dihydro-1H-dibenzo[b,e] azepine; and finally, carrying out cyclization on the 6-(aminomethyl)-6,11-dihydro-1H-dibenzo[b,e] azepine and cyanogen bromide to obtain the epinastine. The synthesis method disclosed by the invention avoids the application of expensive and flammable lithium aluminium hydride and aluminium hydride as well as hypertoxic sodium cyanide, so that the operation is safer in industrial production, and the cost is reduced. The method is simple in process and high in yield, requires mild conditions, and is suitable for industrialized production.
Synthesis method of epinastine
Synthesis method of epinastine
Synthesis method of epinastine
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Owner:GUANGZHOU INST OF BIOMEDICINE & HEALTH CHINESE ACAD OF SCI

Preparation method of epinastine hydrochloride and intermediate thereof

InactiveCN103509025AHigh purityHigh yieldOrganic chemistryBenzeneEpinastine Hydrochloride
Preparation method of epinastine hydrochloride and intermediate thereof
Preparation method of epinastine hydrochloride and intermediate thereof
Preparation method of epinastine hydrochloride and intermediate thereof
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Owner:YAOPHARMA CO LTD +1

Heteroaryl pyridone and aza-pyridone amide compounds

ActiveUS20150011461A1Nervous disorderDipeptide ingredientsIn vivoAza Compounds
Heteroaryl pyridone and aza-pyridone amide compounds
Heteroaryl pyridone and aza-pyridone amide compounds
Heteroaryl pyridone and aza-pyridone amide compounds
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Owner:GENENTECH INC

Collecting agent comprising ammoniated compounds (primary, secondary, tertiary amines), for use in the process of grinding and/or floating copper, molybdenum, zinc, and other contained mineral ores

ActiveUS7299930B2Organic chemistryTransportation and packagingManganeseSodium sulfate
The present invention provides a ammoniated collector (amine, azepine, etc.) alone or in combination with other thiol-type collecting reactants, as well as sodium, iron, magnesium, and / or manganese sulfates, sulfurs, oxides, and hydroxides, acrylic acid polymers and copolymers or other spreading agents, in the process of grinding and floating mineral ores, in order to allow to set new floating operational conditions in existing mineral ore processing plants; to obtain substantial improvements in metallurgic productivity by improving the kinetics of the floating process, which allows to increase recovery of molybdenum, decrease recovery of iron, increase copper grade in copper concentrate, at least keep or improve copper recovery, among others, through the addition of a collecting reactant implying savings of up to 100% of consumption of modifying agents, such as lime, currently used.
Collecting agent comprising ammoniated compounds (primary, secondary, tertiary amines), for use in the process of grinding and/or floating copper, molybdenum, zinc, and other contained mineral ores
Collecting agent comprising ammoniated compounds (primary, secondary, tertiary amines), for use in the process of grinding and/or floating copper, molybdenum, zinc, and other contained mineral ores
Collecting agent comprising ammoniated compounds (primary, secondary, tertiary amines), for use in the process of grinding and/or floating copper, molybdenum, zinc, and other contained mineral ores
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Owner:PROCESOS MINEROS E IND CONOSUR

Asymmetric catalytic reduction of oxcarbazepine

ActiveUS8288532B2High substrate concentrationOptimize volumeAntibacterial agentsNervous disorderHydrogenAlkaline earth metal
A process for preparing (S)-(+)-10,11-dihydro-10-hydroxy-5H-dibenz / b,f / azepine-5-carboxamide or (R)-(−)-10,11-dihydro-10-hydroxy-5H-dibenz / b,f / azepine-5-carboxamide, by reduction of oxcarbazepine in the presence of a catalyst and a hydride source is disclosed. The catalyst is prepared from a combination of [RuX2(L)]2 wherein X is chlorine, bromine or iodine, and L is an aryl or aryl-aliphatic ligand, with a ligand of formula (A) or formula (B):wherein R1 is chosen from C1-6 alkoxy and C1-6 alkyl, n is a number from 0 to 5, and when n is a number from 2 to 5, R1 can be the same or different, and R2 is alkyl, substituted alkyl, aryl, substituted aryl, alkaryl or substituted alkaryl. The hydride source is either NR3R4R5 and formic acid, [R3R4R5NH][OOCH] and optionally formic acid, or [M][OOCH]x and formic acid, wherein R3, R4 and R5 are C1-6 alkyl, M is an alkali metal or alkaline earth metal and x is 1 or 2. A pH from 6.5 to 8 is maintained during the process.
Asymmetric catalytic reduction of oxcarbazepine
Asymmetric catalytic reduction of oxcarbazepine
Asymmetric catalytic reduction of oxcarbazepine
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Owner:BIAL PORTELA & CA SA

Preparation method for 7-chlorine-5-oxo-2,3,4,5-tetrahydro-1H-1-benzoazepine

ActiveCN102329268AHigh purityShort reaction timeOrganic chemistryArginineReaction step
The invention relates to a preparation method for 7-chlorine-5-oxo-2,3,4,5-tetrahydro-1H-1-benzoazepine. The 7-chlorine-5-oxo-2,3,4,5-tetrahydro-1H-1-benzoazepine is an important intermediate for preparing arginine pitressin V2 receptor antagonist Tolvaptan. In the preparation method, the target product 7-chlorine-5-oxo-2,3,4,5-tetrahydro-1H-1-benzoazepine is prepared by removing tosyl and carbalkoxy from 7-chlorine-5-oxo-4-carbalkoxy-1-tosyl-2,3,4,5-tetrahydro-1-benzoazepine serving as a raw material under the action of sulfuric acid and by a 'one-pot method'. The sulfuric acid is used for performing 'one-pot method' reaction, so reaction steps are reduced and reaction time is greatly shortened. The preparation method has the advantages of simpleness and convenience for operation, equipment and cost saving, simpleness and practicability in separation and purification, short reaction time, high yield and high product purity and is applicable to industrialized production.
Preparation method for 7-chlorine-5-oxo-2,3,4,5-tetrahydro-1H-1-benzoazepine
Preparation method for 7-chlorine-5-oxo-2,3,4,5-tetrahydro-1H-1-benzoazepine
Preparation method for 7-chlorine-5-oxo-2,3,4,5-tetrahydro-1H-1-benzoazepine
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Owner:TIANJIN INSTITUTE OF PHARMA RESEARCH

Preparation method of tolvaptan

InactiveCN106883175AEasy to operateHigh yieldOrganic chemistryIndustrial waste waterKetone
The invention discloses a preparation method of tolvaptan. According to the preparation method, 7-chloro-1,2,3,4-tetrahydrobenzo[b]azepine-5-one and 4-nitro-2-methyl bromobenzene are taken as the primary raw materials; high purity tolvaptan is obtained after steps of carbonyl inserting reactions, reduction reactions, and acylation reactions, and the yield is high. The preparation method has the advantages that no bromine or tin dichloride is used; the preparation method does not generate a large amount of industrial waste water, and the environment is protected. At the same time, the generation of impurities namely a compound V and a compound VIII is avoided, and the purification becomes easier. No explosive, flammable, and toxic solvent such as chloroform, ether, and the like, is used, the requirements on the protection of workers are lowered, and the safe production is guaranteed. Moreover, the route design is novel, the raw materials are easily available, the operation of the technology is simple and feasible, and a simple and feasible method is provided for the massive industrial production of tolvaptan.
Preparation method of tolvaptan
Preparation method of tolvaptan
Preparation method of tolvaptan
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Owner:天津泰普制药有限公司

Fused azepine derivatives and their use as antidiuretic agents

InactiveUS7176195B2BiocideNervous disorderAgonistAVP - Arginine vasopressin
Fused azepine derivatives and their use as antidiuretic agents
Fused azepine derivatives and their use as antidiuretic agents
Fused azepine derivatives and their use as antidiuretic agents
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Owner:VANTIA

Novel Compounds

InactiveUS20070293477A1Useful in treatmentBiocideSenses disorderArylAlkoxy group
This invention relates to novel compounds useful in the treatment of diseases associated with TRPV4 channel receptor. More specifically, this invention relates to certain substituted amino-azepines, according to Formula I Specifically, the invention is directed to compounds according to Formula I wherein: R1 is optionally substituted C3-7cycloalkyl, optionally substituted C3-7cycloalkenyl, optionally substituted Het-C3-7alkyl, optionally substituted Het-C3-7alkenyl, optionally substituted aryl, optionally substituted heterocycloalkyl, optionally substituted heteroaryl, or optionally substituted indenyl; R2 is H, optionally substituted C1-6alkyl, C3-6cycloalkyl-C0-6alkyl, Ar—C0-6alkyl, or Het-C0-6alkyl; each R3 is independently H, optionally substituted C1-8alkyl, optionally substituted C2-8alkenyl, optionally substituted C2-8alkynyl, Het-C1-6 alkyl, optionally substituted C3-6cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl, or optionally substituted heteroaryl, or optionally substituted C1-C6 alkoxy; R4 is H, or optionally substituted C1-C4 alkyl; R5 is H, optionally substituted C1-8alkyl, optionally substituted C2-8alkenyl, optionally substituted C2-8alkynyl, optionally substituted C3-6cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl, or optionally substituted heteroaryl; R6 is H or C1-6alkyl; and X is SO2, CO, CH2, or CONH, and pharmaceutically acceptable salts, hydrates, solvates and pro-drugs thereof.
Novel Compounds
Novel Compounds
Novel Compounds
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Owner:SMITHKLINE BECKMAN CORP

Synthesis method of 10-oxa-10,11-dihydro-5H-dibenzo(b,f) azepine

ActiveCN101781249AReduce dosageReduce pollutionOrganic chemistrySynthesis methodsReaction step
The invention relates to a synthesis method of 10-oxa-10,11-dihydro-5H-dibenzo(b,f) azepine shown in the formula (I). The synthesis method comprises the following steps of: carrying out oxidizing reaction at 0-200 DEG C by taking 10,11-dihydro-5H-dibenzo(b,f) azepine shown in the formula (II) as a raw material, nitroxides shown in the formula (III) as a catalyst, acetate as a catalyst promoter, calcium hypochlorite as an oxidant and inorganic salt as a carrier, and after reaction, processing reaction liquid to obtain the 10-oxa-10,11-dihydro-5H-dibenzo(b,f) azepine shown in the formula (I). The invention has the advantages of short reaction step, high conversion rate and yield, advanced process path, mild reaction conditions, small catalyst consumption, no use of brom-containing reagent like NBS (N-bromosuccinimide), liquid bromine and the like, simple after-treatment and less pollution to the environment.
Synthesis method of 10-oxa-10,11-dihydro-5H-dibenzo(b,f) azepine
Synthesis method of 10-oxa-10,11-dihydro-5H-dibenzo(b,f) azepine
Synthesis method of 10-oxa-10,11-dihydro-5H-dibenzo(b,f) azepine
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Owner:ZHEJIANG UNIV OF TECH +1

Method for racemization of (S)-(+)- and (R)-(-)-10,11-dihydro-10-hydroxy-5h-dibenz[B,F]azepine-5-carboxamide and optically enriched mixtures thereof

ActiveUS7189846B2High yieldHigh purityBiocideNervous disorderFormamideRacemization
Method for racemization of (S)-(+)- and (R)-(-)-10,11-dihydro-10-hydroxy-5h-dibenz[B,F]azepine-5-carboxamide and optically enriched mixtures thereof
Method for racemization of (S)-(+)- and (R)-(-)-10,11-dihydro-10-hydroxy-5h-dibenz[B,F]azepine-5-carboxamide and optically enriched mixtures thereof
Method for racemization of (S)-(+)- and (R)-(-)-10,11-dihydro-10-hydroxy-5h-dibenz[B,F]azepine-5-carboxamide and optically enriched mixtures thereof
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Owner:BIAL PORTELA & CA SA

Chemical synthetic method of azepine derivate

ActiveCN101302198AHigh yieldReasonable process conditionsOrganic chemistryChemical synthesisHydrolysate
The invention discloses a synthesis method for an azepine derivative, in particular relating to a chemical synthesis method for 10-oxa-10,11-dihydro-5H-dibenzo[b,f]azepin-5-formylamino. The method of the invention is as follows: 10-cyano-10,11-dihydro-5H-dibenzo[b,f]azepin-5- formylamino undergoes bromination at the benzyl position to give a bromide. The bromide undergoes hydrolysis to give a hydrolysate which is oxidized under the condition of NaClO / TEMPO to give a carboxide. And finally a cyan in the carboxide is hydrolyzed by H2O2 in an alkaline condition to give the resultant. The method has the advantages of reasonable process condition, cheap materials, convenient and rapid operation, highly improved resultant yield, giving far more environment-friendly process due to the hydrolysis of cyan with hydrogen peroxide compared with that with concentrated sulphuric acid, having large advantages for industrial production. The method can be widely used in pharmaceutical industry.
Chemical synthetic method of azepine derivate
Chemical synthetic method of azepine derivate
Chemical synthetic method of azepine derivate
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Owner:浙江瑞博制药有限公司

Novel process for preparation of 10-oxo-10, 11-dihydro-5h-dibenz [b,f] azepine-5-carbox- amide (oxcarbazepine) via intermediate, 10-methoxy-5h-debenz[b,f] azepine-5-carbonyl- chloride

InactiveUS20070032647A1Inhibition formationReduce the temperatureOrganic chemistryOrganic baseBis(trichloromethyl) carbonate
A process for preparation of 10-oxo-10,11-dihydro-5H-dibenz[b,f]azepine-5-carboxamide (oxcarbazepine) via intermediate 10-methoxy-5H-dibenz[b,f]azepine-5-carbonyl chloride, comprising the steps: a) Preparation of an intermediate 10-methoxy-5H-dibenz[b,f]azepine-5 carbonyl, chloride from 10-methoxyiminostillbene using bis (trichloromethyl) carbonate (BTC) with organic base such as aliphatic or aromatic tertiary amines in organic solvent; b) Conversion of the intermediate to 10-methoxy-5H-dibenz[b,f]azepine-5-carboxamide using ammonia in organic solvent; c) Formation of oxcarbazepine from step (b) using Bronsted acid in an organic solvent at a temperature between 25° C.-80° C., preferably at 50° C. to 70° C.; and d) Isolation of oxcarbazepine.
Novel process for preparation of 10-oxo-10, 11-dihydro-5h-dibenz [b,f] azepine-5-carbox- amide (oxcarbazepine) via intermediate, 10-methoxy-5h-debenz[b,f] azepine-5-carbonyl- chloride
Novel process for preparation of 10-oxo-10, 11-dihydro-5h-dibenz [b,f] azepine-5-carbox- amide (oxcarbazepine) via intermediate, 10-methoxy-5h-debenz[b,f] azepine-5-carbonyl- chloride
Novel process for preparation of 10-oxo-10, 11-dihydro-5h-dibenz [b,f] azepine-5-carbox- amide (oxcarbazepine) via intermediate, 10-methoxy-5h-debenz[b,f] azepine-5-carbonyl- chloride
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Owner:AMOLI ORGANICS LTD

Synthesis method of azepine anthraquinone

InactiveCN101712648AAchieve synthesisHas antibacterial activityOrganic chemistryPlatinum saltsIsomerization
The invention relates to a synthesis method of azepine anthraquinone. The azepine anthraquinone is obtained by carrying out intramolecular 6-endo-dig cycloisomerisation reaction shown as in formula (1) on N-propargyl quinine with a 1,5-eneyne structure under the action of a metal catalyst, and purifying, wherein the intramolecular 6-endo-dig cycloisomerisation reaction is homogeneous phase metal catalytic reaction, the metal catalyst is gold salt, platinum salt or univalent gold complex; and the use level of the metal catalyst is 0.01-0.5 equivalent weight of the N--propargyl quinine. The gold slat is auri chloridum (AuCl3) or aurous chloride (AuCl); the platinum salt is platinum tetrachloride, platinum bichloride or potassium chloroplatinate; and the univalent gold complex is PPh3AuOTf, PPh3AuSbF6, PPh3AuNTf2 or LAuNTf2, wherein L is nitrogen heterocyclic ring carbene ligand. The invention realizes the synthesis of the azepine anthraquinone by utilizing metal catalytic intramolecular eneyne cyclization reaction, and has the advantages of simple and easy-accessible raw materials and moderate reaction conditions.
Synthesis method of azepine anthraquinone
Synthesis method of azepine anthraquinone
Synthesis method of azepine anthraquinone
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Owner:NANJING UNIV

Azepine brazilin compound and synthesis method thereof

InactiveCN101798284AOrganic active ingredientsOrganic chemistrySynthesis methodsBlood sugar
The invention relates to an azepine brazilin compound and a synthesis method thereof. By using the structure of a natural product brazilin as a simulation object, a series of brazilin structure compounds containing nitrogen atoms are designed; and substituted cinnamic acid is used as a raw material, and a series of azepine brazilin compounds is obtained through serial chemical conversion and synthesis. Partial azepine brazilin compounds have strong anti-cancer activity, partial compounds have anti-HIV (Human Immunodeficiency Virus) activity, and partial compounds have aldose reductase suppressive activity and obviously reduce the blood sugar level. Medical compositions prepared from the compounds and at least one pharmaceutically acceptable excipient or carrier can be used for treating cancer and resist virus infections.
Azepine brazilin compound and synthesis method thereof
Azepine brazilin compound and synthesis method thereof
Azepine brazilin compound and synthesis method thereof
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Owner:YUNNAN UNIV

Preparation method of alcaftadine intermediate

ActiveCN103408549AAvoid introducingEasy to operateOrganic chemistryKetoneGrignard reaction
The invention provides a preparation method of 6,11-dihydro-11-(1-methyl-4-subpiperidyl)-5H-imidazole[2,1-b][3] benzo azepine shown in a formula (I). The preparation method comprises the following steps of: with N-methyl-4-piperidine formyl chloride hydrochloride and 1-phenethyl-1H-imidazole as raw materials, carrying out an acylation reaction under the action of alkali to obtain [1-(2- phenethyl)-1H-imidazole-2-yl] (1-methyl-4-piperidyl) ketone, and then synthesizing 6,11-dihydro-11-(1-methyl-4-subpiperidyl)-5H-imidazole[2,1-b][3] benzo azepine. The invention provides a simple and efficient preparation method of 6,11-dihydro-11-(1-methyl-4-subpiperidyl)-5H-imidazole[2,1-b][3] benzo azepine, the preparation method is short in route and easy in operation, and can be used for avoiding a grignard reaction and introduction of precious metal, greatly shortening the existing reaction route and greatly increasing the reaction yield.
Preparation method of alcaftadine intermediate
Preparation method of alcaftadine intermediate
Preparation method of alcaftadine intermediate
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Owner:SHANGHAI PUKANG PHARMA

Methods for the stereoselective synthesis of substituted piperidines

InactiveUS20020177721A1Organic chemistryDiseaseCombinatorial chemistry
One aspect of the present invention relates to methods of synthesizing substituted piperidines. A second aspect of the present invention relates to stereoselective methods of synthesizing substituted piperidines. The methods of the present invention will find use in the synthesis of compounds useful for treatment of numerous ailments, conditions and diseases that afflict mammals, including but not limited to addiction and pain. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the substituted piperidines using the methods of the present invention. An additional aspect of the present invention relates to enantiomerically substituted pyrrolidines, piperidines, and azepines.
Methods for the stereoselective synthesis of substituted piperidines
Methods for the stereoselective synthesis of substituted piperidines
Methods for the stereoselective synthesis of substituted piperidines
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Owner:SEPACOR INC

Substituted piperazines of azepines, oxazepines and thiazepines

InactiveUS20060270656A1Improved adverse event profileGood dopamine D bindingBiocideNervous disorderThiazepineHalogen
Described herein are antipyschotic compounds of formula (I)
wherein:
is an optionally benzo-fused five or six member aromatic ring having zero to three hetero atoms independently selected from N, O, and S;
    • R1 is hydrogen, (C1-6) fluoroalkyl, (C3-6) cycloalkyl, or (C1-4) alkyl, wherein the (C1-4) alkyl is unsubstituted or substituted with hydroxy, methoxy, ethoxy, OCH2CH2OH, —CN, imidazolidin-2-one, phenyl, or tetrazole wherein tetrazole is unsubstituted or substituted with (C1-4) alkyl;
    • R2 is H, halogen, (C1-6) fluoroalkyl, (C3-6) cycloalkyl, OR6, SR6, NO2, CN, COR6, C(O)OR6, C(OH)R6, CONR7R8, phenyl or (C1-6) alkyl, wherein the (C1-6) alkyl is unsubstituted or substituted with a hydroxy;
    • R3 is hydrogen, (C1-6)fluoroalkyl , (C3-6) cycloalkyl, (C2-6) alkenyl, phenyl, monocyclic heteroaromatic, bicyclic heteroaromatic, or (C1-4)alkyl wherein (C1-4) alkyl is unsubstituted or substituted with a phenyl;
    • R4 and R5 are independently selected from hydrogen, halogen, (C1-6) alkyl, (C1-6) fluoroalkyl, OR9, SR9, NO2, CN, or COR9;
    • R6 is hydrogen, (C1-6) fluoroalkyl, or (C1-6) alkyl;
    • R7 and R8 are independently hydrogen, or (C1-6) alkyl;
    • R9 is hydrogen, (C1-6) fluoroalkyl, (C1-6) alkyl;
    • Alk is (C1-4) alkylene unsubstituted or substituted with a hydroxy;
    • Y is oxygen, sulfur, SO2, or a bond;
    • X is CH2, C═O, S, O, or SO2;
    • Z is hydrogen, halogen, (C1-6) alkyl, (C1-6)fluoroalkyl, —OH, (C1-6) alkoxy, (C1-6) fluoroalkoxy, (C1-6) alkylthio, (C1-6) acyl, (C1-4)alkylsulfonyl, —OCF3, —NO2, —CN, carboxamido which may be substituted on the nitrogen by one or two (C1-4) alkyl groups, and —NH2 in which one of the hydrogens may be replaced by a (C1-4) alkyl group and the other hydrogen may be replaced by either a (C1-4) alkyl group, a (C1-6) acyl group, or a (C1-4) alkylsulfonyl group;
    • the phenyl of R1, R2 or R3 is independently unsubstituted or substituted with one to three substituents independently selected from Z;
    • the monocyclic heteroaromatic of R3 is unsubstituted or substituted with one to three substituents independently selected from Z;
    • the bicyclic heteroaromatic of R3 is unsubstituted or substituted with one to three substituents independently selected from Z; and salts, solvates, and crystal forms thereof.
Also described are the use of the compounds of formula (I) as antagonists of the dopamine D2 receptor and as agents for the treatment of psychosis and bipolar disorders, and pharmaceutical formulations of the compounds of formula (I).
Substituted piperazines of azepines, oxazepines and thiazepines
Substituted piperazines of azepines, oxazepines and thiazepines
Substituted piperazines of azepines, oxazepines and thiazepines
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Owner:ELI LILLY & CO

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