102 results about "Hydroxy derivative" patented technology

The present invention relates to novel pyrrolo[2,1-c][1,4]benzodiazepines compounds of general formula V as shown below, which are useful as potential antitumour agents and a process of preparing these compounds; particularly the present invention provides a process for the preparation of 7-methoxy-8-{n-[7-methoxy-(11aS)-1,2,3,10,11,11a-hexahydro-5H-pyrrolo[2,1-c][1,4]ben-zodiazepine-5-one-8-yloxy]alkyloxy}-(11aS)-1,2,3,11a-tetrahydro-5H-pyrrolo[2,1-c][1,4]benzodiazepin-5-one, with varying aliphatic chain length and its 2-hydroxy derivatives.

The present invention discloses a kind of amphiphilic BAB-type block copolymer with polyglycol blocks at two ends and polyhexanolactone section in the middle part and its preparation process and application. It is prepared with diisocyanate as cross-linking agent polyglycol or other single- or double-hydroxy derivative and polycaprolactone glycol as material. The copolymer can self-assemble in water into nanometer particle or micelle with shell of hydrophobic polydexanolactone section and shell of hydrophilic polyglycol. It has excellent coating capacity to hydrophobic medicine and thus may be used in preparing water soluble nanometer particle or micelle of hydrophobic medicine.

The present invention provides a novel compound represented by the general formula I;wherein R is H or COR3;R1 is H, R2, phenyl, or COR3, wherein R2 is C1-C5 lower alkyl and R3 is R2 or phenyl;Z is CH2 or O;Y is OH or OCOR3;x is 0 or 1; andX is C1-C5 n-alkyl, C3-C7 cycloalkyl, phenyl, furanyl, thienyl or substituted derivatives thereof, wherein the substituents maybe selected from the group consisting of C1-C5 alkyl, halogen, CF3, CN, NO2, NR42, CO2R4 and OR4 wherein R4 is hydrogen or C1-C5 alkyl and dotted lines represent the presence or absence of a double bond and wavy lines represent a cis or trans bond. These novel compounds are especially useful for treating elevated intraocular pressure (ocular hypertension) and glaucoma.

The present invention describes a process for the industrial production of L-carnitine, comprising the enantioselective reduction of an alkyl 4-chloro-3-oxobutyrate or 4-chloro-3-oxobutyramide. The optically active 3-hydroxy derivative thus obtained is reacted with trimethylamine, obtaining crude L-carnitine, which is then finally purified. The catalyst used for the reduction is a complex of ruthenium bound to a penta-atomic bis-heteroaromatic system. The reduction reaction, performed in controlled conditions of hydrogen pressure, substrate concentration, temperature, and substrate: catalyst molar ratio, enables 4-chloro-3-hydoxybutyrate or 4-chloro-hydroxybutyamide to be obtained in a high yield. The process described, which leads to L-carnitine being obtained, is easily applicable on an industrial scale.

The present invention provides a synthetic process for the N-demethylation of N-methyl morphinans. In particular, the invention provides improved synthetic methods for the preparation of N-demethylated morphinan compounds that may be employed as starting materials, for example, commonly available N-methyl opiates such as oripavine and thebaine, and C(3)-protected hydroxy derivatives of oripavine.

It was found that a fluoro derivative can be produced by reacting a hydroxy derivative with sulfuryl fluoride (SO2F2) in the presence of an organic base or in the presence of an organic base and “a salt or complex comprising an organic base and hydrogen fluoride”. According to the present production process, it is not necessary to use perfluoroalkanesulfonyl fluoride, which is not preferable in industrial use, and it is possible to advantageously produce optically-active fluoro derivatives, which are important intermediates of medicines, agricultural chemicals and optical materials, specifically 4-fluoroproline derivatives, 2′-deoxy-2′-fluorouridine derivatives, optically-active α-fluorocarboxylate derivatives, and the like, even in a large scale.

The invention discloses a preparation method of self-assembled superlattice materials of a titanium dioxide nano rod, comprising the following steps: (1) monodispersed TiO2 nano rods are synthetized, and the synthetic reaction is based on a condition that an unstable hydroxy derivative is produced by oleic acid titanium under nucleophillic attack of oil amide, the hydroxy derivative can be further polymerized to generate Ti-o-Ti, and produced TiO2 nano sticks are dispersed to a non-polar solvent to make clear TiO2 solution; (2) superfluous oil acid surface activators are added into the solution, and the superlattice materials with different structures (riband shapes and beehive shapes) are made by controlling the concentration of the oil acid in the solution and evaporating slow solvents. The invention has the advantages of firstly expanding the preparation scope of one-dimensional superlattice materials to the TiO2 nano rods of anatase, utilizing superfluous oil acid surface active agent to lead depletion attraction to adjacent TiO2 nano sticks, thereby adding macro-control factors for self-assembled drive force of the nano sticks so as to enable the self-assembled behavior to be easily generated.

The present invention describes a process for the industrial production of L-carnitine, comprising the enantioselective reduction of an alkyl 4-chloro-3-oxobutyrate or 4-chloro-3-oxobutyramide. The optically active 3-hydroxy derivative thus obtained is reacted with trimethylamine, obtaining crude L-carnitine, which is then finally purified. The catalyst used for the reduction is a complex of ruthenium bound to a penta-atomic bis-heteroaromatic system. The reduction reaction, performed in controlled conditions of hydrogen pressure, substrate concentration, temperature, and substrate: catalyst molar ratio, enables 4-chloro-3-hydoxybutyrate or 4-chloro-hydroxybutyamide to be obtained in a high yield. The process described, which leads to L-carnitine being obtained, is easily applicable on an industrial scale.

This invention refers to the synthesis and purification of 2 hydroxide derivatives of fatty acids, as well as to the separation method of its enantiomers (or optic isomers) [−] y [+], to the enantiomers themselves, to pharmaceutical compositions which include them, and to their use as medicines, as well as to an in vitro method of diagnosis / prognosis and evaluation of the potential use of the molecules of the invention in different pathologies, as well as their use for the regulation of certain enzymes and the study of their activity and effects.

The present invention provides a novel compound represented by the general formula I:wherein R is H or COR3;R1 is H, R2, phenyl, or COR3, wherein R2 is C1-C5 lower alkyl and R3 is R2 or phenyl;Z is CH2 or O;Y is OH, OCOR3 or =O;x is 0 or 1; andX is C1-C5 n-alkyl, C3-C7 cycloalkyl, phenyl, furanyl, thienyl or substituted derivatives thereof, wherein the substituents maybe selected from the group consisting of C1-C5 alkyl, halogen, CF3, CN, NO2, NR42, CO2R4 and OR4 wherein R4 is hydrogen or C1-C5 alkyl and dotted lines represent the presence or absence of a double bond and wavy lines represent a cis or trans bond. These novel compounds are especially useful for treating elevated intraocular pressure (ocular hypertension) and glaucoma.

Process for the preparation of phenol and cyclohexanone which comprises:a. the synthesis of cyclohexylbenzene by the hydro-alkylation of benzene by contact with hydrogen or the alkylation of benzene with cyclohexene using Y zeolites;b. the selective aerobic oxidation of cyclohexylbenzene to the corresponding hydroperoxide catalyzed by N-hydroxy-derivatives in the presence of polar solvents; andc. the scission of the hydroperoxide of cyclohexylbenzene to phenol and cyclohexanone by homogeneous or heterogeneous acid catalysts;characterized in that the synthesis of cyclohexylbenzene takes place in the presence of a catalytic system comprising a Y zeolite and an inorganic ligand wherein the Y zeolite has a crystalline structure with openings consisting of 12 tetrahedra and the inorganic ligand is γ-alumina, and wherein said catalytic composition is characterized by a pore volume, obtained by adding the mesoporosity and macroporosity fractions, greater than or equal to 0.7 cm3 / g, wherein at least 30% of said volume consists of pores with a diameter greater than 100 nanometers.

The invention discloses a preparation method of 7-ketone sterides. The preparation method comprises the following steps: 1, firstly, dissolving steroids and an N-hydroxyl derivative as a catalyst in a solvent, then adding an oxidizing agent to generate an allylic oxidation reaction at a temperature of 0-60 DEG C, after the sterides are completely oxidized, ending the reaction, wherein the mol ratio of the sterides to the N-hydroxyl derivative as the catalyst is 1:(0.1-10), and the mol ratio of the sterides to the oxidizing agent is 1:(2-10); 2, drying a solvent in a reaction solution obtained in the step 1 by distillation, and then recovering the N-hydroxyl derivative as the catalyst through normal hexane to obtain the 7-ketone sterides.

Provided herein are enzymatic methods of producing steroid compounds such as 7-dehydropregnenolone, hydroxy derivatives thereof and vitamin D2- and D3-like compounds and derivatives thereof. Also provided are the derivatives of the vitamin D3-like compounds so generated via the action of cytochrome P450scc enzyme on substrates 7-dehydrocholesterol, vitamin D2 or vitamin D3.