Process for the sulfinylation of a pyrazole derivative

C - Chemistry – Metallurgy – 07 – D

Patent

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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 2667559

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 selected from trifluoromethylsulfinic acid, trifluoromethylsulfinic acid anhydride, and a trifluoromethylsulfinate alkaline or alkaline earth metal salt and mixtures of the acid and/or the salt(s), in the presence of at least one amine acid complex wherein the amine(s) are selected from 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.

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 choisi parmi l'acide trifluorométhylsulfinique, l'anhydride d'acide trifluorométhylsulfinique et un sel de métal alcalin ou alcalino-terreux de trifluorométhylsulfinate ainsi que des mélanges de l'acide et/ou du ou des sels, en présence d'au moins un complexe d'acides aminés, la ou les amines étant choisies parmi des amines tertiaires, le ou les acides étant choisis parmi l'acide fluorhydrique, chlorhydrique, bromhydrique et iodhydrique et des dérivés d'acide sulfonique. Ledit procédé consiste en outre à ajouter un agent halogénant.

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