Abstract: The invention relates to a process for preparation of the compound 3-methyl-5-benzyloxy-2-(4-benzyloxyphenyl)-1H-indole 5, an intermediate for the synthesis of bazedoxifene and bazedoxifene acetate.

Abstract: The invention relates to a process for preparation of the compound 3-methyl-5-benzyloxy-2-(4-benzyloxyphenyl)-1H-indole 5, an intermediate for the synthesis of bazedoxifene and bazedoxifene acetate.

Abstract: Disclosed is a process for the preparation of toltrazuril of formula (I) via the intermediate N-methyl-N?-[3-methyl-4-[4-[(trifluoromethyl)thio]phenoxy]phenyl] imidodicarbonic diamide of formula (III) wherein intermediate (III) is obtained via a novel intermediate without the use of potentially hazardous reagents or potentially unstable intermediates.

Abstract: The present invention describes a process for the synthesis of ursodeoxycholic acid wherein the purification of the crude ursodeoxycholic acid (containing approximately 13-15% of chenodeoxycholic acid impurity) takes place first passing through a salification with imidazole and a subsequent purification via “methyl ester”, which allows a finished product with an extremely low content of known “cheno and “litho” impurities to be obtained. The present invention also describes the recovery steps of cholic acid and 3?-hydroxy-7-ketocholanic acid from the mother liquors of process intermediates.

Abstract: The present invention relates, in a first aspect, to a process preparing vilazodone hydrochloride that comprises the reaction of 3-(4-chloro-1-hydroxy-butyl)-1H-indol-5-carbonitrile with 5-piperazin-1-yl-benzofuran-2-carboxylate methyl hydrochloride with the formation of a 1,4-piperazine, with subsequent dehydration, hydrogenation and treatment with ammonia, to obtain vilazodone in free base form that is then converted into the hydrochloride thereof.

Abstract: The present invention relates, in a first aspect, to a process preparing vilazodone hydrochloride that comprises the reaction of 3-(4-chloro-1-hydroxy-butyl)-1H-indol-5-carbonitrile with 5-piperazin-1-yl-benzofuran-2-carboxylate methyl hydrochloride with the formation of a 1,4-piperazine, with subsequent dehydration, hydrogenation and treatment with ammonia, to obtain vilazodone in free base form that is then converted into the hydrochloride thereof.

Abstract: There is described a process for the preparation of cinacalcet hydrochloride (I) which includes the steps of: a) reacting (R)-(+)-1-(1-naphthyl)ethylamine (II) with 3-[3-(trifluoromethyl)phenyl]propenaldehyde (III) to afford the non isolated intermediate (R)—N-[3-[3-(trifluoromethyl)phenyl]-2-propenylimino-N-[1-(1-naphthyl)ethylamine (IV); b) reducing the non isolated intermediate (R)—N-[3-[3-(trifluoromethyl)phenyl]-2-propenylimino-N-[-1-(1-naphthyl)ethylamine (IV) with a sequential addition of:—a solution of sodium borohydride, methanol and a base,—oxalic acid and—a base to obtain (R)—N-[3-[3-(tifluoromethyl)phenyl]-2-propenyl]-1-(1-naphthyl)ethylamine (V) by passing through the precipitation of the oxalate salt of compound (V) after the addition of oxalic acid; c) hydrogenating (R)—N-[3-[3-(trifluoromethyl)phenyl]-2-propenyl]-1-(1-naphthyl)ethylamine (V) thus obtaining (R)—N-(3-(3-(trifluoromethyl)phenyl]propyl]-1-(1-naphthyl)ethylamine cinacalcet base (VI), which is retaken in ethyl acetate; and d) treati

Abstract: The present invention relates, in a first aspect, to a process preparing vilazodone hydrochloride that comprises the reaction of 3-(4-chloro-1-hydroxy-butyl)-1H-indol-5-carbonitrile with 5-piperazin-1-yl-benzofuran-2-carboxylate methyl hydrochloride with the formation of a 1,4-piperazine, with subsequent dehydration, hydrogenation and treatment with ammonia, to obtain vilazodone in free base form that is then converted into the hydrochloride thereof.

Abstract: Process for preparing 2-methoxycarbonylmethyl-6,6-dimethyl-2-tetrahydropyran carboxylic acid (I) comprising: a) Reaction of 5-bromo-2-methyl-2-pentene (III) with magnesium and then diethyloxalate to obtain ethyl-2-oxo-6-methyl-5-heptenoate (IV); b) Reaction of ethyl-2-oxo-6-methyl-5-heptenoate (IV) with an alkali amide and methyl acetate to obtain ethyl-2-methoxycarbonylmethyl-2-hydroxy-6-methyl-5-heptenoate (V); c) Reaction of ethyl-2-methoxycarbonylmethyl-2-hydroxy-6-methyl-5-heptenoate (V) with an alkali metal hydroxide to obtain the corresponding 2-carboxymethyl-2-hydroxy-6-methyl-5-heptenoic acid (VI); d) Cyclisation of 2-carboxymethyl-2-hydroxy-6-methyl-5-heptenoic acid (VI) with formic acid to give 2-carboxymethyl-6,6-dimethyl-2-tetrahydropyrancarboxylic acid (VII); e) Monoesterification of 2-carboxymethyl-6,6-dimethyl-2-tetrahydropyrancarboxylic acid (VII) to 2-methoxycarbonylmethyl-6,6-dimethyl-2-tetrahydropyran carboxylic acid (I), characterised in that in stage (e) the 2-methoxycarbonylmethyl-6,6

Abstract: A process for the preparation of 4-[2-(5-ethyl-2-pyridyl)ethoxy]nitrobenzene is described, which comprises the step of reacting 2-(5-ethyl-2-pyridyl)ethanol with 1-fluoro-4-nitrobenzene in acetone in the presence of an alkali metal hydroxide. The intermediate 4-[2-(5-ethyl-2-pyridyl)ethoxy]nitrobenzene is used for the preparation of pioglitazone.

Abstract: Process for preparing 3?-7?(?)-di-hydroxy-6?(?)-alkyl-5?-cholanic acid (I) in which R is a linear or branched C1-C5 alkyl and the relative intermediates 3?-hydroxy-6?-alkyl-7-keto-5?-cholanic (VIII) and 3?-hydroxy-6?-alkyl-7-keto-5?-cholanic (IX).

Abstract: A conversion process of gabapentin hydrochloride into gabapentin comprising: a) dissolution of gabapentin hydrochloride in a solvent in which the gabapentin hydrochloride and the gabapentin are completely soluble; and b) subsequent addition of an amine that allows the removal of the chloride ion from the solution containing gabapentin hydrochloride, by precipitation of the hydrochloride of the same amine, leaving the gabapentin in solution in free amino acid form.

Abstract: Synthetic process of isobutyl methyl 1,4,-dihydro-2,6-dimethyl-4-(2-nitrophenyl)3,5-pyridine dicarboxylate (Nisoldipine) comprising on the reaction of isobutyl 2-(2-nitrobenzylidene)acetoacetate with methyl 3-aminocrotonate in an apolar solvent.

Abstract: A process for synthesis of 1-(aminomethyl)cyclohexane acetic acid hydrochloride (Gabapentin hydrochloride) comprising: a) Reaction of a mixture of acetic anhydride/ammonium acetate with 1,1-cyclohexane-diacetic acid to yield 3,3-pentamethylene glutarimide; b) Treatment of 3,3-pentamethylene glutarimide with sodium hydroxide in an aqueous solution up to dissolution, dripping the solution thus obtained into a sodium hydroxide/sodium hypochlorite mixture, which is also aqueous, followed by acidification with hydrochloric acid to yield gabapentine hydrochloride.

Abstract: A process for synthesis of 1-(aminomethyl)cyclohexane acetic acid hydrochloride (Gabapentin hydrochloride) comprising:

Abstract: Process for the preparation of ipriflavone consisting in the following steps:a) reaction of 2,4-dihydroxy-phenyl-benzyl-ketone of formula (II) with ethyl orthoformate in dimethylformamide as solvent and in the presence of a catalyst consisting of morpholine, to yield 7-hydroxyisoflavone of formula (III),b) separation of product (III) from the reaction residue,c) alkylation of product (III) from step b) with isopropyl halide to obtain ipriflavone, wherein:I. step a) is carried out at a temperature ranging from 115 to 120.degree. C. using a 2,4-dihydroxy-phenyl-benzyl-ketone (II) weight/solvent volume (w/v) ratio lower than 1:4;II. step b) consists in the precipitation of the corresponding salt with dicyclohexylamine of formula (IV).The process yields 7-hydroxyisoflavone (III) in high yields within short reaction times (2 h max.) and ipriflavone with impurity .ltoreq.0.1%.

Abstract: Process for the preparation of derivatives having general formula (I) ##STR1## wherein the meaning of R will be defined in the text, characterized by the reaction between a compound having formula ##STR2## wherein X is an halogen, and an alkaline salt of a methyl dialkylmalonate.

Abstract: Salification products between cholic acids (chenodeoxicholic and ursodeoxycholic acid) and trimebutyne in the molar ratio 1:1 or 2:1 have been prepared. These new salts show a pharmacotherapeutic action, which, as a whole, is not found in other known drugs, and which makes them useful for the treatment of diskinesiae, biliary dyspepsiae, cholecystopathies, and for the normalization of the kinesis of the intestinal gastro-biliary tract.

Abstract: A process for preparing very pure ursodeoxycholic acid starting from cholic acid (I) by:(a) selectively oxidizing it to 3 alpha, 12 alpha-dihydroxy-7-ketocholanic acid (II)(b) reducing acid (II) to 3 alpha, 7 beta, 12 alpha-trihydroxy-cholanic acid (III)(c) oxidizing a 3,7-ester of acid (III) to 3 alpha, 7 beta-dihydroxy-12-keto-5-beta-cholanic acid (IV) by treatment with hypochlorite followed by hydrolysis(d) preparing the tris-trimethylsilyl derivative of acid (IV)(e) eliminating the trimethylsilyl groups(f) reducing the very pure acid (IV) by the Wolff-Kishner method to ursodeoxycholic acid.Alternatively, the Wolff-Kishner method can be applied directly to the tris-trimethylsilyl derivative, and the trimethylsilyl groups can be eliminated from the final product.

Abstract: A process for preparing 3.alpha., 7.beta.-dihydroxy-cholanic acid (I) from 3.alpha., 7.alpha.-dihydroxy-.DELTA..sub.11 -cholenic acid. This starting substance is converted by oxidation and successive reduction into 3.alpha., 7.beta.-dihydroxy-.DELTA..sub.11 -cholenic acid, which is separated in the form of the tris-trimethylsilyl derivative of high purity. The product (I) is obtained by hydrogenating and hydrolyzing the trisilyl derivative.