72 results about "Isocoumarin" patented technology

The present invention discloses a class of isocoumarin derivatives, which have the following general formula, wherein R is selected from hydrogen atom, C1-C10 alkyl, halogen, carbonyl, hydroxyl, nitrile, ester, alkoxy or trifluoromethoxyl, and E1 or E2 is selected from C1-C6 alkyl formate, phenyl or nitrile. The present invention further discloses a synthesis method of the isocoumarin derivatives. According to the present invention, divalent copper is adopted as a catalyst, a simple and easily-available o-halogenated benzoic acid and an alkyne compound are adopted as starting raw materials to synthesize an isocoumarin compound and derivatives thereof, and advantages of low cost, high yield, simple operation, easily-available raw materials, simple reaction equipment, easy industrial production, and the like are provided.

The invention discloses a synthetic method of non-natural 3, 4- dihydro-isocoumarin derivant and intermediate compound and usage in agricultural chemicals domain, which is characterized by the following: possessing chemical constitution general formula as follow; comprising six 3, 4- dihydro-isocoumarin derivant (C series). This invention discloses the synthetic method of this compound, usage and purposes.

The invention discloses a novel isocoumarin compound. The isocoumarin compound has the chemical name of 2-(hydroxymethyl)-8,8-dimethyl-9,10-dihydropyrano[4,3-f]benzopyran-4 (8H)-one, the molecular formula of C15H16O4 and the structure represented by a formula shown in the specification. The invention further discloses a preparation method for preparing the isocoumarin compound from tobacco. The invention further discloses use of the compound, and shown by activity tests, the compound plays a good role in inhibiting tobacco mosaic virus. The compound disclosed by the invention is simple in structure and relatively good in tobacco mosaic virus resisting activity and can be applied to the research and development of tobacco mosaic virus resisting pesticide preparations as a tobacco mosaic virus resisting lead compound.

The present invention relates to a new phosphonic isocoumarin salt and a preparation method. The compound of the present invention has a molecular formula shown on the right, wherein, R = alkyl of R = H, C1-10, naphthenic base of C3-7, aryl, the substituted derivatives; Z = Li, Na, K, Rb, Cs; Y = H, alkyl of C1-4, alkoxyl, carbonyl, halogen, CN, CF3, NO2, OH, amidocyanogen, aryl; X = H, C1, Br, I, alkyl of C1-10, naphthenic base of C3-7, aryl, the substituted derivatives. The phosphonic isocoumarin salt is prepared by the reaction of phosphonic isocoumarin ester under the function of alkali metal salt. The phosphonic isocoumarin salt of the present invention has certain water solubility and can be applied to the related fields of enzyme inhibitors, anti-rumor, etc.

The invention provides compound cockroach glucosides A to C and a drug composition thereof and their application in preparation of pharmaceuticals and health-care products for treating ulcers and burns and scalds. Ulcers and burns are fairly common, and American cockroaches clinically used for various ulcers and burns have a good effect. Three dihydrogen isocoumarin glucosides are separated and identified and are named as the cockroach glucosides A, B and C, and all the cockroach glucosides can promote dermal fibroblast collagen secretion of human and improve the treatment effect on the collagen secretion lack diseases, such as all kinds of ulcers, burns and scalds.

The present invention relates to a preparation method for synthesizing non-natural isocoumarin, its 3,4-dihydroderivative and its intermediate. Said invention provides the application of isocoumarin, its 3,4-dihydroderivative and its intermediate in the fields of agricultural pesticide and medicine. Said invention also provides their structure formulae.

The invention discloses a method for preparing isocoumarin and derivatives thereof, comprising the following steps of: putting an o-halogen benzoic acid, a 1, 3-dicarbonyl compound, cuprous salt and alkali in a reaction vessel, adding a dimethyl formamide (DMF) solvent into the reaction vessel, hermetically stirring at a temperature of 100-120 DEG C, reacting for 12-24 hours, quenching the reaction, extracting, washing, drying, concentrating and purifying the reaction liquid and obtaining an end product. The synthetic method of the isocoumarin and the derivatives thereof is scientific and reasonable and has the characteristics of high synthetic yield, good selectivity, easiness in purifying the products and the like; and the isocoumarin derivatives with various substituent groups, which cannot be synthetized by utilizing the other methods, can be synthetized and obtained.

The invention discloses an isocoumarin compound and a preparation method and an application thereof. The isocoumarin compound is separated from canella tailed spicebush root and leaf (Lindera caudata) and is named caudacoumarin A; the English name is caudacoumarin A; the molecular formula of the caudacoumarin A is C16H18O5; and the caudacoumarin A has the following structure as shown in the specification. The preparation method of the isocoumarin compound comprises the following steps: with canella tailed spicebush root and leaf as a raw material, extractum extraction, organic solvent extraction, MCI decoloration, column chromatography on silica gel, and high-pressure liquid chromatography separation. The application is an application of the isocoumarin compound in preparation of an anti-mosaic virus medicine. Through a test by a half-leaf method, the caudacoumarin A displays good anti-tobacco mosaic virus activity. The isocoumarin compound disclosed by the invention is simple in structure and good in activity, can be used as a lead compound of resisting the tobacco mosaic virus, and has a relatively good application prospect.

The invention discloses an isocoumarin compound as well as a preparation method and application of the isocoumarin compound as a natural marine organism antifouling agent. The isocoumarin compound is characterized in that the compound has a structure as shown in formula I, wherein R2 and R2 independently represent H and a structure as shown in specification, and R1 or R2 is H; and R3 and R4 independently represent H and OCH3, and R3 or R4 is H. The compound as shown in formula I can be prepared through adopting such means as cultivation, fermentation and chromatographic separation on marine fungi, i.e., Eurotium sp. (HM991283). The natural marine organism antifouling agent disclosed by the invention is efficient and low in toxicity, and is characterized in that the compound of formula I or salt thereof, as an active ingredient, is used for preventing and controlling marine organism fouling caused by barnacle.

The invention discloses a multi-substituent isocoumarin derivative and a preparation method thereof. According to the preparation method, substituted tert-butyl peroxybenzoate represented by a formula II, 1,2-disubstituted acetylene represented by a formula III, a catalyst, alkali, acid and a solvent are uniformly mixed and are heated under the protection of nitrogen for a cyclization reaction, and a compound represented by a general structure formula I is obtained after the reaction. According to the method, the reaction conditions are mild, the reaction time is short, the substrate range is wide, the reaction specificity is high, the yield is high, the post-processing is simple and convenient, and the multi-substituent isocoumarin derivative which cannot be synthesized with other methods can be synthesized and has a wide application.

The invention discloses a synthesis method of an isocoumarin derivative. The method comprises the following steps: adding 3-hexyl-4-cyan-6,7-dimethoxy isocoumarin (A), a cuprous catalyst and acetaldoxime (B) in a reaction vessel, adding a solvent N,N-dimethyl formamide (DMF), stirring and refluxing; reacting for 1 hour, cooling, filtering reaction solution in vacuum, and adding a certain amount of water in the filtrate, filtering separated solid in vacuum, drying and low-temperature crystalizing obtained coarse product so as to obtain a target product 3-hexyl-4-acylamoni-6,7-dimethoxy isocoumarin (C). The method for translating the isocoumarin into acylamino is scientific and reasonable, the step is simple, the reaction time is short, the selectivity is good, the translation rate is high, the product is easy to purify; cuprous salt is firstly used as the catalyst, and the catalysis efficiency is high in comparison with the reported cupric, in particular, the cuprous has good catalysis effect on cyan hydrolysis with large steric hindrance.

The invention discloses an isocoumarin compound, which is named as 5-((E)-4-hydroxy-3-methyl-butyl-3-ene)-3-(hydroxymethyl)-1H-isochromen-6-ol and has a molecular formula of C15H18O4. The structure of the isocoumarin compound is described in the specification. The invention also discloses a preparation method and application of the isocoumarin compound. Experiments prove that the isocoumarin compound provided by the invention is capable of improving the smoking quality of cigarettes; and through mixing of the isocoumarin compound with a moisture-retaining agent according to a proper ratio, good physical and sensory moisture-retaining effects are exerted on cigarettes, the smoke of cigarettes can be softened, the mellow and full sensation and amenity of the smoke of cigarettes can be improved, and the smoke of cigarettes is endowed with delicate fragrance.

The invention provides an ailanthus flower extract as well as a preparation method and an application of active ingredients brevifolin of the ailanthus flower extract. The ailanthus flower extract and a total isocoumarin active part are prepared through researching the chemical components of ailanthus flower, and three types of cyclopentanone isocoumarin, i.e. brevifolin, brevifolin-carboxylic acid and methyl brevifolincarboxylat are obtained through separation. A biological activity research shows that the ailanthus flower extract has the remarkable anti-oxidation, anti-inflammation and anti-tumor effects. Experimental results show that the ailanthus flower extract (including effective part) and ailanthus flower elements with active compounds can be used for preparing drugs and health care products for oxidation resistance, inflammation resistance, tumor resistance and other relevant diseases treatment.

The invention discloses an isocoumarin compound. The isocoumarin compound has the chemical name of 3,5-bis(hydroxymethyl)-6-methoxy-1H-isobenzopyran-1-one, the molecular formula of C12H12O5 and the structure represented by a formula shown in the specification. The invention further discloses use of the compound, and shown by activity tests, the compound plays a good role in inhibiting tobacco mosaic virus. The compound disclosed by the invention is simple in structure and relatively good in tobacco mosaic virus resisting activity and can be applied to the research and development of tobacco mosaic virus resisting pesticide preparations as a tobacco mosaic virus resisting lead compound.

A method of preparing optically active isocoumarin-3-yl-acetic acid derivatives represented by Formula (I): wherein a specific isocoumarin-ketene derivative is subjected to an addition reaction with an optically active alcohol, and then the ester thus obtained is subjected to a hydrolysis reaction. An intermediate for synthesis used therein. A method of preparing isocoumarin-3-yl-acetic acid derivatives represented by Formula (III): wherein a specific isocoumarin derivative is subjected to an addition reaction with carbon monoxide and oxygen in the presence of a transition metal catalyst. An intermediate for synthesis used therein.

The invention discloses a synthesis method of isocoumarin compounds. According to the method, benzaldehyde compounds and alkyne compounds are taken as reaction materials, and the isocoumarin compoundsare prepared under the condition of a cobalt catalyst with PEG-400 as a reaction medium. The method has the advantages that the catalysis conditions are novel, the catalyst cost is low, the catalystand the reaction medium PEG-400 can be recycled, the application range of a reaction substrate is wide, the yield is high, and the method is environmentally friendly.

The invention discloses a synthetic method of isocoumarin ramification. The synthetic method comprises the following steps that a raw material 2-((2-R2)-ethynyl) methyl benzoate (II) is dissolved in dimethyl sulfoxide or deuterium dimethyl sulfoxide, and is dropped in thionyl chloride and reacts to obtain isocoumarin ramification (I). The synthetic method has the advantages that operation is easy,the raw material is cheap and easy to obtain, reaction condition is mild, reaction time is short, and the yield is ideal.

The invention discloses a method for preparing isoquinoline ketone and derivatives thereof, comprising the following steps of: placing o-halogen benzamide, a 1, 3-dicarbonyl compound, cuprous salt and alkali into a reaction vessel, adding a dimethyl formamide (DMF) or toluene as a solvent into the reaction vessel, hermetically stirring at a temperature of 100-120 DEG C for reacting for 12-36 hours, and quenching the reaction, extracting, washing, drying, concentrating and purifying the reaction liquid to obtain an end product. The synthetic method of the isoquinoline ketone and the derivatives thereof is scientific and reasonable and has the characteristics of high synthetic yield, good selectivity, easiness in purifying the product and the like; and the isoquinoline ketone derivatives with various substituent groups, which cannot be synthetized by utilizing the other methods, can be synthetized and obtained.

The invention discloses a method for synthesizing an isocoumarin compound through electrochemical oxidative dehydrogenation coupling, and belongs to the technical field of organic chemistry. In a non-separated electrolytic tank, substituted aryl formic acid 1 and an alkyne compound 2 are subjected to a constant-current electrolytic reaction in an organic solvent in the presence of an iridium catalyst and an additive to obtain an isocoumarin derivative 3. According to the method disclosed by the invention, a C-O / O-H bond cyclization product is obtained with high selectivity under the condition of electric anodic oxidation and the catalysis of transition metal iridium. The method is mild in reaction condition, environment-friendly, high in yield and good in purity, and a simple and effective synthesis way is provided for the isocoumarin compound.

The invention discloses a preparation method for substituted isocoumarin derivatives. The method comprises the following steps: a novel carbon-carbon bond and a carbon-oxygen bond are constructed while a carbon-carbon bond and a carbon-hydrogen bond are cut, a base, dichloro(p-cymene)ruthenium(II) dimer, 2,4,6-trimethylbenzoic acid and sulfur ylide are reacted in an organic solvent, and thereforethe substituted isocoumarin derivatives are prepared. According to the method provided by the invention, the raw materials used in the method are easy to obtain, the yield is high, the reaction conditions are mild, the reaction time is short, the substrate range is wide, the reaction specificity is strong, and the post-treatment is simple and green.

The invention discloses a method for synthesizing 3-alkynyl isocoumarins compounds. 2-(2, 2-ethylene dibromide) benzoic acid derivatives and terminal alkyne compounds are used as raw materials for the3-alkynyl isocoumarins compounds, bivalent palladium and univalent copper are used as catalysts, and tri-aryl phosphine compounds and alkali are used as additives. The method includes carrying out heating reaction in organic solvents to synthesize a series of 3-alkynyl isocoumarins compounds. A chemical reaction formula is shown. The method has the advantages of simple steps, mild conditions, short reaction time, high atom economy, easily available raw materials, environmental friendliness and the like. Besides, the 3-alkynyl isocoumarins compounds are a type of important bioactive moleculesand synthetic intermediates, and accordingly the method can be widely applied to the field of medicine synthesis and has high use value and a high social benefit.

The present invention provides a preparation method for isocoumarin compounds. The method comprises the following steps: using 2-arylbenzaldehyde represented by a formula I in the description as a rawmaterial, performing a reaction at the temperature of 0-50 DEG C for 6-36h in an organic solvent under the actions of a copper catalyst, an oxidant and alkaline matter, and performing separation purification on an obtained reaction liquid to obtain the isocoumarin compounds represented by a formula II in the description. According to the invention, the raw materials are cheap and easy to obtain,the reaction conditions are mild, the tolerance of the functional groups is good, the operation is simple and environmentally friendly, and a novel method is provided for synthesizing isocoumarin containing various substituent groups.

A process for making perillyl alcohol is disclosed. The process comprises isomerizing a starting material comprising trans-isocarveol at a temperature within the range of 100° C. to 220° C. in the presence of a Group 5 metal catalyst to produce perillyl alcohol. We surprisingly found that trans-isocarveol, which can be selectively produced from a commercially available mixture of cis- and trans-LMO, can be isomerized directly to perillyl alcohol. Yields of perillyl alcohol are improved when the isomerization is performed under an inert atmosphere and / or in the presence of a phenolic antioxidant. Performing the isomerization in the presence of a high-boiling alcohol and / or distilling the perillyl alcohol product from the reaction mixture in the presence of a high-boiling alcohol, enhances yields and maximizes catalyst use. The resulting distillation residue, which contains recovered Group 5 metal catalyst, is valuable for catalyzing additional trans-isocarveol isomerizations.

The invention discloses a chlorinated isocoumarin derivative and a preparation method and an application thereof, which belong to the field of biochemical industry. A molecular formula of the derivative is C16H14Cl2O7, and a structural formula is shown in a specification. The preparation method comprises the following steps: myoporum bontioides endophytic fungi Trichoderma sp. 09 is subjected to bacterial strain cultivation in a bacterial strain medium, the bacterial strain is subjected to fermentation cultivation in a fermentation medium, the obtained mycelia is subjected to extraction by ethanol-water or methanol-water, and then is performed with vacuum concentration, the mycelia is extracted by an organic solvent extraction; an extract is concentrated and is subjected to column chromatography on silica gel and Sephdex LH-20 gel column chromatography, an eluate is concentrated and recrystallized to obtain the white crystals which are the chlorinated isocoumarin derivative. The chlorinated isocoumarin derivative has strong effect for inhibiting gloeosporium musarum and rice sheath blight fungus and can be used as a microbe agricultural bactericide, the raw materials enable large scale production, and the application prospect is wide.

A method for enhancing the efficacy of chemotherapy in the treatment of cancer in animals, particularly humans, is provided wherein isocoumarin derivatives that exhibit unique chemopotentiation properties are employed in a combination treatment with chemotherapy.

The invention discloses a preparation method of an isocoumarin derivative shown as a formula III. The formula III is shown in the description, wherein R1 and R2 are independently selected from one of hydrogen group, phenyl, C1 to C3 linear alkyl and C3 branched alkyl respectively; R3, R4 and R6 are independently selected from one of hydrogen group, hydroxyl, C1 to C3 linear alkyl, C3 branched alkyl, methoxyl and phenyl respectively; R5 is selected from halogeno, nitryl, halogenated methyl, phenyl and halogenated phenyl; R7, R8, R9, R10, R11 and R12 are independently selected from one of halogeno, nitryl, C1 to C3 linear alkyl, C3 branched alkyl, methoxyl, phenyl and halogenated phenyl respectively. Compared with the prior art, the method has the advantages that reaction raw materials are cheap and easy to obtain and the stability is relatively high; the yield of reaction products is high, side reactions are few and post-treatment of reaction is simple; various starting raw materials can be selected and the same target molecule is obtained.

The invention discloses a method for synthesizing an isocoumarin compound through electrochemical oxidative dehydrogenation coupling, and belongs to the technical field of organic chemistry. In a non-separated electrolytic tank, substituted aryl formic acid 1 and an alkyne compound 2 are subjected to a constant-current electrolytic reaction in an organic solvent in the presence of an iridium catalyst and an additive, and an isocoumarin derivative 3 is obtained. According to the method disclosed by the invention, a C-O / O-H bond cyclization product is obtained with high selectivity under the condition of electric anodic oxidation and the catalysis of transition metal iridium; and the method is mild in reaction condition, environment-friendly, high in yield and good in purity, and a simple and effective synthesis way is provided for the isocoumarin compound.