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 2667565

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 secondary and/or tertiary amines and the acid(s) are selected from hydrofluoric, hydrochloric, hydrobromic and hydroiodic acid and 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, wherein the temperature of the reaction mixture at no time exceeds 39°C.

La présente invention concerne un procédé permettant la sulfinylation d'un dérivé pyrazole, caractérisé en ce que du 5-amino-1-[2,6-dichloro-4-(trifluorométhyl)phényl]-1H-pyrazole-3-carbonitrile (II) est mis à réagir avec un agent de sulfinylation S en présence d'au moins un complexe d'amine(s) et d'acide(s), l'amine ou les amines étant choisies parmi des amines secondaires et/ou tertiaires et l'acide ou les acides étant choisis parmi l'acide fluorhydrique, chlorhydrique, bromhydrique et iodhydrique et des dérivés d'acide sulfonique, et avec l'addition d'un agent d'halogénation, où S représente [CF3S(O)]2O ; où CF3S(O)X où X signifie un groupe fluoro, chloro, bromo, iodo, hydroxy, ou un sel de métal alcalin ou alcalino-terreux du groupe hydroxy ; ou leurs mélanges, la température du mélange réactionnel ne dépassant à aucun moment 39 °C.

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