Chemical process for the production of sulphinyl derivatives...

C - Chemistry – Metallurgy – 07 – D

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C07D 401/12 (2006.01)

Patent

CA 2323422

A process for the preparation of a compound of formula (I) in which R1, R2, R3 and R4 represent: a) (R1=CH3; R2=OCH3; R3=CH3; R4=OCH3) or b) (R1=CH3; R2=OCH2CF3; R3=H; R4=H) or c) (R1=OCH3; R2=OCH3; R3=H and R4=OCHF2) respectively and pharmaceutically acceptable salts thereof, comprising reacting a compound of formula (II) in which R1, R2, R3 and R4 represent a) (R1=CH3; R2=OCH3; R3=CH3, R4=OCH3) or b) (R1=CH3; R2=OCH2CF3; R3=H; R4=H) or c) R1=OCH3; R2=OCH3; R3=H and R4=OCHF2) respectively, with a perborate salt in a liquid diluent at a pH in the range of 7.5 to 14 at a temperature in the range of 0 ~C to the boiling point of the liquid diluent employed.

L'invention concerne un procédé pour la préparation d'un composé de formule (I), dans laquelle R¿1?, R¿2?, R¿3? et R¿4? représentent a) (R¿1?=CH¿3?; R¿2?=OCH¿3?; R¿3?=CH¿3?; R¿4?=OCH¿3?) ou b) (R¿1?=CH¿3?; R¿2?=OCH¿2?CF¿3?; R¿3?=H; R¿4?=H) ou c) (R¿1?=OCH¿3?; R¿2?=OCH¿3?; R¿3?=H; R¿4?=OCHF¿2?) respectivement et les sels pharmaceutiquement acceptables associés. Ce procédé consiste à faire réagir un composé de formule (II), dans laquelle R¿1?, R¿2?, R¿3? et R¿4? représentent a) (R¿1?=CH¿3?; R¿2?=OCH¿3?; R¿3?=CH¿3?; R¿4?=OCH¿3?) ou b) (R¿1?=CH¿3?; R¿2?=OCH¿2?CF¿3?; R¿3?=H; R¿4?=H) ou c) (R¿1?=OCH¿3?; R¿2?=OCH¿3?; R¿3?=H; R¿4?=OCHF¿2?) respectivement avec un sel de perborate dans un diluant liquide à un pH allant de 7,5 à 14 à une température comprise entre 0 ·C et le point d'ébullition du diluant liquide utilisé.

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