Zach System

Pcas Biosolution

Juliette Martin

Alain Burgos

Sylvie Blanchet

Blandine Bertrand

Sonia Roussiasse

Florence Perrin

Yvon Derrien

Laurent Fourage

Denis Wahler

Gerard Guillamot

Jean-François Pluvie

Françoise Bourdeau

The invention relates to an enzymatic acylation method including at least the following steps of: contacting at least one compound having at least one function selected from among the amine, alcohol, or thiol functions, at least one microorganism having an acyl transfer activity and/or an acyl transfer enzyme, and at least one acylphosphonate donor of formula (I), where: R is an alkyl, alkene, alkyne, aryl, or aralkyl radical, or is &#x2014;ORa, &#x2014;SRa, &#x2014;NRaRb, where Ra and Rb are identical or different and are H, an alkyl, alkene, alkyne, aryl or aralkyl radical, the alkyl, alkene, alkyne, aryl or aralkyl radicals being optionally substituted; X is O or S; Y and Z, which are identical or different, are &#x2014;OR1, &#x2014;OR2, &#x2014;SR1, &#x2014;SR2, &#x2014;NR'1R&#x2033;1, &#x2014;NR&#x2032;2R&#x2033;2; R1, R2, R&#x2032;1, R&#x2032;2, R&#x2033;1 and R&#x2033;2, which are identical or different, are an alkyl, alkene, alkyne, aryl or aralkyl radical, said alkyl, alkene, alkyne, aryl or aralkyl radicals being optionally substituted; and recovering the compound including at least one acyl function, said function being selected from among the amine, alcohol, or thiol functions. 

Enzymatic acylation method using an acylphosphonate donor

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

Growing community of inventors

Aramon, France

Juliette Martin