Synthelabo

Lydia Zard

Thomas A Purcell

Arlette Tixidre

Guy Rossey

Pascal George

Samir Jegham

Jonathan Reid Frost

Jean-Claude Muller

Alexander E Wick

Daniel J Galtier

Frederic Puech

Philippe Burnier

Corinne Rousselle

Patrick Pasau

Andre Bourbon

Regine Bartsch

Jean Jacques Koenig

Jacques Comarmond

Luc Rivron

Howard Williams

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.

Process for the resolution of ethyl

Process for the preparation of one or both enantiomers of 1-(4-chlorophenyl)-2-chloroethanol, which comprises an enantioselective enzymatic hydrolysis of (.+-.)-.alpha.-(4-chlorophenyl)chloroethyl acetate by means of an enzyme which is horse liver acetone powder, lipase PS from Pseudomonas fluorescens, lipase AK from Pseudomonas or the lipase from Candida antarctica, to give a mixture of unhydrolysed R-(-)-.alpha.-(4-chlorophenyl)chloroethyl acetate and S-(+)-1-(4-chlorophenyl)-2-chloroethanol, and optional separation of R-(-)-.alpha.-(4-chlorophenyl)chloroethyl acetate and optional hydrolysis of it to give R-(-)-1-(4-chlorophenyl)-2-chloroethanol and use of the enantiomers of 1-(4-chlorophenyl)-2-chlorethanol for the preparation of the enantiomers of eliprodil and of their salts.

Enantiomeric separation of (RS)1-(4-chlorophenyl)-2-chloroethanol by

3,3a,4,5-Tetrahydro-1H-oxazolo[3,4-a]quinolin-1-one derivatives of formula (I) ##STR1## in which: n is 0 or 1,

Oxazoloquinolinone derivatives, their preparation and their therapeutic

Compounds of the formula ##STR1## in which Y represents hydrogen, fluorine, chlorine, methyl or methoxy, R.sub.1 represents phenyl substituted by fluorine, methyl, methoxy, trifluoromethyl or phenyl, or R.sub.1 represents 2-thienyl, R.sub.2 represents methyl, and R.sub.3 represents (C.sub.1 -C.sub.4)-alkyl, or phenyl-(C.sub.1 -C.sub.2)-alkyl optionally substituted on the ring by 2 to 3 methoxy groups, or 2-(2-pyridyl)ethyl, or R.sub.2 and R.sub.3 form, with the adjacent nitrogen, 4-phenyl(1-piperidyl), 4-phenylmethyl(1-piperidyl), 1,2,3,4-tetrahydro-2-isoquinolyl, 6-methoxy-1,2,3,4-tetrahydro-2-isoquinolyl, 5,8-dimethoxy-1,2,3,4-tetrahydro-2-isoquinolyl, 6,7-dimethoxy 1,2,3,4-tetrahydro-2-isoquinolyl, 2,3,4,5-tetrahydro-1H-3-benzazepin-3-yl, or 7,8-dimethoxy-2,3,4,5-tetrahydro-1H-3-benzazepin-3-yl, and X represents carbonyl or sulphonyl, and their salts are useful as neuroprotective and antiiischaemic agents.

Benzoxazine derivatives and their application in therapy

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.

Process for the preparation of methyl

A compound which is an N-(imidazolymethyl) diphenylazomethine derivative of the general formula (I) ##STR1## wherein R.sub.1 is chlorine or methyl,

N-(imidazolylmethyl)diphenylazomethines and compositions containing them

A compound, in the form of a pure optical isomer or a racemate, which is a dibenzo[be]oxepinacetic acid of the general formula (I) ##STR1## in which R1, R2 and R3, which may be the same or different, each represent hydrogen or methyl, XX represents a carbon-carbon bond or two hydrogen atoms, and YY represents a carbon-carbon bond or two hydrogen atoms, or a pharmaceutically acceptable salt thereof has useful therapeutic properties, especially as an anti-inflammatory.

Dibenzo[b,e]oxepinacetic acid derivatives and pharmaceutical

Compounds of general formula ##STR1## in which R.sub.1, taken separately, denotes a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group, and

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Gif sur Yvette, France

Lydia Zard