Zach System

Teva Pharmaceutical Industries Limited

Atopix Therapeutics Limited

Sylvie Blanchet

Alain Burgos

Yvon Derrien

Juliette Martin

Blandine Bertrand

Sonia Roussiasse

Florence Perrin

Jean-François Pluvie

Jacques Tonnel

Françoise Bourdeau

Bertrand Blandine

Guillaume Léonard Pierre Dewaele

Marie-Laure Moreau

Jaques Tonnel

The invention relates to an industrial scale process for the preparation of a compound of general formula (I): (Formula (I)) wherein R, Rand Rare as defined herein. The process comprises reacting compounds of general formulae (II) and (III): (formulae (II), (III)) in the presence of a Lewis acid followed by a reduction with triethylsilane.

Process for the preparation of 3-substituted (indol-1-yl)-acetic acid esters

A process for the production of ene-amide derivatives represented by the formula (I) wherein R1 and R2 and R3 are independently a hydrogen atom, an alkyl, a cycloalkyl, a cycloalkylalkyl, an alkylaryl, an aryl, a heterocycle, a cyano, an alkoxy, an aryloxy, a carboxyl, a carbamoyl, &#x2014;CONR5R6 (in which R5 and R6 are independently an alkyl, arylalkyl or aryl group said ring being substituted or not with a functional group or with R5) or &#x2014;COOR5 group (in which R5 is an alkyl, alkylaryl or aryl group), said alkyl, cycloalkyl, cycloalkylalkyl, alkylaryl and aryl groups being substituted or not with a functional group or with R5; or R1 and R2 taken together, may form a ring (which terms includes mono-, di- and higher polycyclic ring systems); R4 is a hydrogen atom, an alkyl, an aryl, an alkylaryl, said groups are substituted or not with a halogen atom as Cl, Br, or F; X is an oxygen atom or a leaving group and m is an integer 1 or 2; when m is 1 then X is a leaving group; when m is 2 then X is a oxygen atom, which comprise: a hydrogenation/isomerization reaction in presence of a heterogeneous catalyst, of an oxime derivatives of formula (II) wherein R1, R2 and R3 are as defined above with an acyl derivative of formula (III) (R4CO)X wherein R4, m and X are as defined above.

Process for the synthesis of eneamide derivatives

A process for the preparation of optically active substituted alpha-amino-indane derivatives of formula (I), which include: an asymmetric hydrogenation reaction of an en-amide derivative of formula (III) in presence of hydrogen and an optically active catalyst, in order to obtain an amide derivative of formula (II), a hydrolysis reaction of the amide derivative of formula (II) obtained in the previous step, in order to obtain optically active substituted alpha-amino-indane derivatives of formula (I).

Process for the synthesis of substituted alpha-aminoindan derivatives

A process for preparing indanylamine and aminotetralin derivatives from indanone or tetralone oximes by acylating the oximes with an organic anhydride, followed by catalytic hydrogenation in the presence of an organic anhydride with subsequent hydrolysis is described. The process is commercially feasible providing indanylamine and aminotetralin derivatives in high yield that are useful as intermediates in the production of therapeutically active compounds. Also described are novel intermediates, 1-indanone O-acetyl oximes and 1-tetralone O-acetyl oximes.

Process for the synthesis of indanylamine or aminotetralin derivatives and novel intermediates

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Feneu, France

Sylvie Blanchet