Sanofi-Synthelabo

Sanofi

Sanofi-Aventis

Elf Sanofi

Jean-Robert Dormoy

Alain Heymes

Bertrand Castro

Alain Rabion

Andre Bousquet

Andre Mortreux

Mouad Alami

Michel Bouisset

Aldo Previero

Patrice Moreau

Jean-Daniel Andre

G&eacute;rard Cahiez

Eric Riguet

Marc Devocelle

Dominique Goubet

Francine Agbossou

The invention relates to lower-alkyl esters of 3-(3,4-dihalophenyl)-2,6-dioxopiperidine-3-propionic acid derivatives, and to processes for preparing the same.

Alkyl esters of 3-(3,4-dihalophenyl)-2,6-dioxopiperidine-3-propionic acid of use as intermediates

Alkyl esters of 3-(3,4-dihalogenophenyl)-2,6-dioxopiperidine-3-propionic acid of use as intermediates

Methyl-phenyl derivatives, preparation method and use

Method for preparing 4-methyl-biphenyl derivatives

Method for preparing optically active .alpha.-substituted benzyl alcohols

Method for preparing 2-thienylethylamine derivatives

The subject of the invention is 2-(1-bromoethyl)benzo[b]thiophene of formula: ##STR1## as well as a process for the preparation thereof, characterised in that 2-ethylbenzo[b]thiophene is reacted, in a solvent, with a brominating agent in the presence of a free radical initiator, which provides the desired compound, and the use thereof in the preparation of 2-(1-(benzyloxyamino)ethyl)benzo[b]thiophene and of N-hydroxy-N-{1-(benzo[b]thien-2-yl)ethyl}urea. No figure.

Substituted 2-ethylbenzo [b] thiophene, process for preparation thereof

The object of the invention is a process for the preparation of the trans(-) (2R,3S) diastereoisomer of the glycidic esters of general formula: ##STR1## wherein a chlorohydrin of general formula: ##STR2## is reacted with a strong organic base in a suitable solvent and at a temperature between -10.degree. C. and room temperature. Another object of the invention is intermediate compounds cis(+) (2S,3S) 1,5-benzothiazepin-4-one.

Process for the preparation of benzothiazepin-one derivatives

The subject of the present invention is a process for the preparation of isoquinoline derivatives in four steps wherein use is made as synthetic intermediates of organo-lithium compounds or related compounds.

Process for the preparation of isoquinoline derivatives

The invention relates to a process for the preparation of morphinane derivatives of general formula: ##STR1## by demethylation of 3-methoxylated compound with a sulfonic acid selected from methanesulfonic acid and trifluoromethanesulfonic acid in the presence of a sulfide.

Process for the preparation of morphinane derivatives

The invention relates to a process for fixing an electrophilic group in the 2-position of 1H-pyrrolo[3,2-c]pyridine N-protected in the 1-position, process which consists in protecting the 1-position in question with a labile protecting group, reacting the compound so obtained with a lithiation agent selected from a lithium amide and an alkyl lithium at a temperature between -80.degree. C. and -20.degree. C. and in the presence of tetramethylethylenediamine to obtain the corresponding 2-lithio derivative and then condensing the metal derivative so obtained at a temperature between -80.degree. C. and room-temperature with a reagent capable of giving rise to an electrophilic group to form N-protected 1H-pyrrolo[3,2-c]pyridine substituted in the 2-position by an electrophilic group.

1H-pyrrolo [3,2-c]pyrrolidines protected in 1-position useful as

A process for preparing 1H-pyrrolo-[3,2-c]-pyridine or 5-aza-indole in high yield, comprising condensing 3-methyl-4-nitropyridine-1-oxide with a compound having a formula ##STR1## wherein R represents a di-loweralkylamino, morpholino, piperidino or pyrrolidino group and R.sub.1 and R.sub.2, which are the same or different, each represent a loweralkoxy group or a group R as defined; to form an enamine having a formula: ##STR2## wherein R is as define and subjecting the enamine IV to reduction cyclization; the enamines IV are new compounds.

Process for preparing 5-aza-indole and intermediates used in this process

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Sisteron, France

Jean-Robert Dormoy