Zach System

Zach System S.p.a.

Sonia Roussiasse

Alain Burgos

Blandine Bertrand

Sylvie Blanchet

Juliette Martin

Jean-François Pluvie

Florence Perrin

Yvon Derrien

Françoise Bourdeau

Stéphane Frein

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 the in situ preparation of chiral compounds derived from oxazaborolidine-borane complexes, wherein a metal borohydride, a Lewis base and an inorganic acid ester are brought together and an optically active amino alcohol and optionally a halide are then added. The compound obtained is a complex that is useful as a catalyst in asymmetric reduction reactions. The reaction is performed by adding the substance to be reduced, particularly prochiral ketones or ether oximes, in order to synthesize chiral alcohols or chiral amines.

Method for the in situ preparation of chiral compounds derived from oxazaborolidine-borane complexes which are used in asymmetric reduction reactions

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