Produits Chimiques Auxiliaires Et De Synthese

Produits Chimiques Auxiliaries Et De Synthese

Pcas Biosolution

Gerard Guillamot

Jean-Marie Schneider

Jonathan Madec

Sergio Kreimerman

Laurent Fourage

Denis Wahler

Juliette Martin

The present patent application relates to a process for preparing cinacalcet or a pharmaceutically acceptable salt thereof, which comprises reacting 3-trifluoromethylbenzaldehyde having the following formula (II) with the phosphorus-comprising derivative having the following formula (III) in which Rand R, which may be identical or different, are each a (C-C)alkyl group. The present invention also relates to the phosphorus-comprising derivative having the formula (III), to the use thereof and to the process for preparing same. The present invention also relates to the phosphate salt of cinacalcet and to uses thereof.

Process for preparing cinacalcet and pharmaceutically acceptable salts thereof

The present patent application relates to a process for preparing, cinacalcet or a pharmaceutically acceptable salt thereof, which comprises reacting 3-trifluoromethylbenzaldehyde having the following formula (II) with the phosphorus-comprising derivative having the following formula (III) in which Rand R, which may be identical or different, are each a (C-C)alkyl group. The present invention also relates to the phosphorus-comprising derivative having the formula (III), to the use thereof and to the process for preparing same. The present invention also relates to the phosphate salt of cinacalcet and to uses thereof.

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

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Viroflay, France

Gerard Guillamot