Abstract: The present invention relates to a novel process for preparing the compound 4-(cyclopropylmethoxy)-N-(3,5-di-chloro-1-oxido-4-pyridyl)-5-methoxypyridine-2-carboxamide of formula (1), in base or hydrate form or in the form of pharmaceutically acceptable salts, and also to several novel synthetic intermediates that are useful in this preparation process.

Abstract: The present invention relates to a novel process for preparing the compound 4-(cyclopropylmethoxy)-N-(3,5-di-chloro-1-oxido-4-pyridyl)-5-methoxypyridine-2-carboxamide of formula (1), in base or hydrate form or in the form of pharmaceutically acceptable salts, and also to several novel synthetic intermediates that are useful in this preparation process.

Abstract: A process for the preparation of ethyl 4,4,4-trifluoro-3(R)-hydroxybutanoate, wherein the ester functional group of the (S) enantiomer of ethyl (.+-.)-4,4,4-trifluoro-3-hydroxybutanoate which comprises (R) and (S) is selectively hydrolysed in aqueous medium, by means of a lipase, and the non-hydrolysed (R) enantiomer is then extracted and used in the preparation of 4,4,4-trifluoro-1,3(R)-butanediol.

Abstract: A compound of formula (1): ##STR1## in which R.sub.1 represents a 1,1-dimethylethyl, triphenylmethyl, methoxymethyl or benzyloxymethyl group; andR.sub.2 represents a C.sub.1 -C.sub.4 alkyl group.

Abstract: A compound represented by formula (V): ##STR1## in which R.sub.1 is selected from the group consisting of hydrogen, unbranched and branched C.sub.1-7 alkyl, unbranched and branched C.sub.3-9 alkenyl, and (C.sub.3-7)cycloalkyl(C.sub.1-6)alkyl groups, and R.sub.2 is selected from the group consisting of hydrogen, unbranched and branched C.sub.1-7 alkyl,(C.sub.3-7)cycloalkyl(C.sub.1-3)alkyl, aryl(C.sub.1-3)alkyl, aryloxy(C.sub.1-3)alkyl, arylthio(C.sub.1-3) alkyl, arylsulphonyl(C.sub.1-3)alkyl and heteroaryl (C.sub.1-3) alkyl groups.

Abstract: Triarylborane derivatives corresponding to the formula (1) ##STR1## in which R either represents a group --CR.sub.1 R.sub.2 R.sub.3 where R.sub.1, R.sub.2 and R.sub.3 are each, independently of one another, a (C.sub.1 -C.sub.2)alkyl or aryl group, or represents a group --CH.sub.2 OR.sub.4 where R.sub.4 is a (C.sub.1 -C.sub.2)alkyl or benzyl group, or represents a group --Si(R.sub.5).sub.3 where R.sub.5 is a (C.sub.1 -C.sub.2)alkyl or aryl group, R being in the 1 or 2 position of the tetrazole ring, their preparation and their use as synthesis intermediates.

Abstract: Derivatives of benzeneborinic acid, preparation thereof and use thereof as synthetic intermediates.

Abstract: Triarylborane derivatives corresponding to the formula (1) ##STR1## in which R either represents a group --CR.sub.1 R.sub.2 R.sub.3 where R.sub.1, R.sub.2 and R.sub.3 are each, independently of one another, a (C.sub.1 -C.sub.2)alkyl or aryl group, or represents a group --CH.sub.2 OR.sub.4 where R.sub.4 is a (C.sub.1 -C.sub.2)alkyl or benzyl group, or represents a group --Si(R.sub.5).sub.3 where R.sub.5 is a (C.sub.1 -C.sub.2)alkyl or aryl group, R being in the 1 or 2 position of the tetrazole ring, their preparation and their use as synthesis intermediates.

Abstract: Compounds corresponding to the formula (I) ##STR1## in which X represents dibromomethyl, formyl, (C.sub.1-4)alkyl, or a group CH(OR.sub.5).sub.2 or CH(OH)OR.sub.5, wherein the or each R.sub.5 is hydrogen (C.sub.1-3)alkyl or the two R.sub.5 's in the case of CH(OR.sub.5).sub.2 are linked to provide a 1,3-dioxolane or 1,3-dioxane ring, and Y represents hydrogen, 1,1-dimethylethyl, triphenylmethyl, trimethylstannyl, tributylstannyl, (1,1-dimethylethyl)dimethylsilyl, (1,1-dimethylethyl)diphenylsilyl, 2-cyanoethyl, or a group CH.sub.2 OR.sub.6 wherein R.sub.6 is methyl, phenylmethyl, 1,1-dimethylethyl, 2,2,2-trichloroethyl, benzyloxycarbonyl or 2,2,2-trichloroethyloxycarbonyl, Y being in position 1 or 2 on the tetrazole ring. The compounds of formula (I) are useful as intermediates in the synthesis of compounds possessing therapeutic activity.

Abstract: A process for preparing a compound represented by formula ##STR1## by deprotecting a compound represented by formula (VII) ##STR2## in which R.sub.1 represents an unbranched or branched C.sub.1-7 alkyl, unbranched or branched C.sub.3-9 alkenyl, or (C.sub.3-7)cycloalkyl(C.sub.1-6)alkyl, and R.sub.2 represents hydrogen, unbranched or branched C.sub.1-7 alkyl, (C.sub.3-7)cycloalkyl(C.sub.1-3)alkyl, aryl(C.sub.1-3)alkyl optionally substituted on the ring-system, aryloxy(C.sub.1-3)alkyl optionally substituted on the ring-system, arylthio(C.sub.1-3)alkyl optionally substituted on the ring-system, arylsulphonyl(C.sub.1-3)alkyl optionally substituted on the ring-system, and heteroaryl(C.sub.1-3)alkyl optionally substituted on the ring-system.

Abstract: Derivatives of benzeneborinic acid corresponding to the formula (1) ##STR1## in which R.sub.1, R.sub.2 and R.sub.3 represent, each independently of the others, either a (C.sub.1 -C.sub.2)alkyl group or an aryl group, the group --CR.sub.1 R.sub.2 R.sub.3 being in position 1 or 2 of the tetrazole ring, preparation thereof, and method of use as synthetic intermediates.

Abstract: A process for the preparation of methyl (-)-(2R,3S)-2,3-epoxy-3-(4-methoxyphenyl)propionate, which comprises subjecting the dextrorotatory (2S,3R) enantiomer, present in a starting mixture containing both the levorotatory (2R,3S and dextrorotatory (2S,3R) enantiomers, to a transesterification reaction, in an anhydrous medium and in the presence of an enzyme which does not affect the levorotatory (2R,3S) enantiomer. The latter is an intermediate for the synthesis of compounds such as Diltiazem.

Abstract: 2-Aminothiophenol is reacted with methyl (-)-(2R,3S)-2,3-epoxy-3-(4-methoxyphenyl)propionate, and the intermediate methyl (2S,3S)-3-[(2-aminophenyl)thio]-2-hydroxy-3-(4-methoxyphenyl)propionate is cyclized in the presence of methanesulfonic acid, in the same vessel and without isolating said intermediate product, using e.g. chlorobenzene as a solvent.

Abstract: Process for the preparation of compounds of the general formula (I) ##STR1## wherein R is hydrogen or (C.sub.1-4)alkyl.

Abstract: 2-Aminothiophenol is reacted with (-)-(2R,3S)-2,3-epoxy-3-(4-methoxyphenyl) methylpropionate, and the intermediate (2S,3S)-3-[(2-aminophenyl)thio]-2-hydroxy-3-(4-methoxyphenyl) methylpropionate is then cyclized in the presence of methane sulfonic acid, in the same container and without isolating said intermediate product, using chlorobenzene as a solvent.

Abstract: A process for the preparation of a methyl (+)-(2S,3S)-3-[(2-aminophenyl)thio]-2-hydroxy-3-(4-methoxyphenyl)propionat e of the formula (I): ##STR1## in which X denotes hydrogen or chlorine, which process comprises reacting a 2-aminothiophenol of formula (II): ##STR2## in which X is as defined above, with methyl (-)-(2R,3S)-2,3-epoxy-3-(4-methoxyphenyl)propionate, in a 1,2-dichloroethane solvent.

Abstract: A compound which is a benzimidazole derivative of formula (I) ##STR1## in which: R.sub.1 is hydrogen or methyl,R.sub.2 is hydrogen, methyl or acetyl,R.sub.3 is hydrogen, methyl or acetyl, andR.sub.4 is hydrogen or a halogen,or a pharmaceutically acceptable acid addition salt thereof.The compounds have histamine antagonist activity and are also synthesis intermediates.

Abstract: A process for the preparation of an imidazopyridine which is a compound of formula (I) ##STR1## in which: Y denotes hydrogen, a halogen or a C.sub.1-4 alkyl group;X.sub.1 and X.sub.2 denote, independently of each other, hydrogen, a halogen or a C.sub.1-4 alkoxy, C.sub.1-6 alkyl, CF.sub.3, CH.sub.3 S, CH.sub.3 SO.sub.2 or NO.sub.2 group; andR.sub.1 and R.sub.2 denote, independently of each other, hydrogen or a C.sub.1-5 alkyl group, with the proviso that R.sub.1 and R.sub.2 do not both denote hydrogen,or a salt thereof;which process comprises reacting a compound of formula (V) ##STR2## wherein Y, X.sub.1, X.sub.2, R.sub.1 and R.sub.2 are as defined above, with a reducing agent and if desired converting the resulting compound of formula (I) into a salt, together with intermediates of formulae: ##STR3## The final products have useful pharmacological properties, e.g. as anxiolytics.

Abstract: Isoquinoline derivatives of the formula (I) ##STR1## in which R is a group selected from t-butyl and groups of the formula ##STR2## and R' is selected from methyl and ethyl, are useful in the preparation of 1(2H)-isoquinolone.

Abstract: 2-Aminothiophenol is reacted with methyl (-)-(2R,3S)-2,3-epoxy-3-(4-methoxyphenyl)propionate, and the intermediate methyl (2S,3S)-3-[(2-aminophenyl)thio]-2-hydroxy-3-(4-methoxyphenyl)propionate is cyclized in the presence of methanesulfonic acid, in the same vessel and without isolating said intermediate product, using e.g. chlorobenzene as a solvent.