Process for the sulfinylation of a pyrazole derivative

Details Process for the sulfinylation of a pyrazole derivative Process for the sulfinylation of a pyrazole derivative

C - Chemistry, Metallurgy

07

D

C07D 231/44 (2006.01) A01N 43/00 (2006.01) A01N 43/56 (2006.01) A61K 31/415 (2006.01) A61P 33/00 (2006.01)

Patent

CA 2667562

The present invention relates to a process for the sulfinylation of a pyrazole derivative, characterized in that 5-amino-1-[2,6-dichloro-4-(trifluoromethyl)phenyl]-1H-pyrazole-3-carbonitrile (II) is reacted with a sulfinylating agent S in the presence of at least one amine acid complex wherein the amine(s) are selected from cyclic secondary amines and the acid(s) are selected from sulfonic acid derivatives, and with the addition of a halogenating agent, wherein S is [CF3S(O)]2O; or CF3S(O)X wherein X means fluoro, chloro, bromo, iodo, a hydroxy group, or an alkaline or alkaline earth metal salt of the hydroxy group; or mixtures thereof.

La présente invention concerne un procédé de sulfinylation d'un dérivé pyrazole, caractérisé en ce qu'on fait réagir un 5-amino-1-[2,6-dichloro-4-(trifluorométhyl)phényl]-1H-pyrazole-3-carbonitrile (II) avec un agent de sulfinylation S en présence d'au moins un complexe d'acides aminés, la ou les amines étant choisies parmi des amines secondaires cycliques et le ou les acides étant choisis parmi des dérivés d'acide sulfonique. Le procédé consiste en outre à ajouter un agent halogénant, S étant [CF3S(O)]2O ou CF3S(O)X, où X signifie fluoro, chloro, bromo, iodo, un groupe hydroxy ou un sel de métal alcalin ou alcalino-terreux du groupe hydroxy, ou des mélanges correspondants.

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