A novel asymmetric synthesis of r and s warfarin and its...

Details A novel asymmetric synthesis of r and s warfarin and its... A novel asymmetric synthesis of r and s warfarin and its...

C - Chemistry, Metallurgy

07

D

C07D 311/56 (2006.01)

Patent

CA 2226752

The present invention provides a novel process for making compounds of formula (2a or 2b) or pharmaceutically acceptable salts thereof, wherein R1 is selected from the group consisting of phenyl and phenyl substituted with at least one group selected from NO2 and halogen, R2 is H; R3 is selected from the group consisting of C1-4 alkyl, phenyl, and benzyl; and, R4 is selected from the group consisting of H and halogen; which comprises the steps of: a) oxidizing a racemate of formula (2) or a salt thereof to form a dehydro-compound of formula (3), wherein R5 is selected from the group consisting of H, CH3, benzyl, C2-8 acyl, Na, Li and K; and, b) asymmetrically hydrogenating a compound of formula (3) in the presence of a chiral phosphine catalyst to form a compound of formula (2a or 2b).

La présente invention se rapporte à un nouveau procédé de fabrication de composés de formule (2a) ou (2b) ou de leurs sels pharmaceutiquement acceptables, dans lesquelles R1 est sélectionné dans le groupe contenant phényle et phényle substitué par au moins un groupe choisi parmi NO2 et hydrogène; R2 représente H; R3 est sélectionné dans le groupe contenant alkyle C1-4, phényle et benzyle; et, R4 est sélectionné dans le groupe contenant H et halogène; le procédé consiste à (a) oxyder un composé racémique de formule (2) ou un de ses sels pour former un composé déhydro de formule (3), dans laquelle R5 est sélectionné dans le groupe contenant H, CH3, benzyle, acyle C2-8, Na, Li et K; et (b) hydrogéner asymétriquement un composé de formule (3) en présence d'un catalyseur de phosphine chirale pour former un composé de formule (2a) ou (2b).

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