Process for the preparation of rapamycin derivatives

Details Process for the preparation of rapamycin derivatives Process for the preparation of rapamycin derivatives

C - Chemistry, Metallurgy

07

D

C07D 498/18 (2006.01)

Patent

CA 2637075

Processes for the production of a 32-deoxorapamycin from a 32-iodo- or 32- hydroxyrapamycin, wherein the hydroxy group is substituted by the residue of an arylthionocarbonate or an arylthiocarbamate, in the presence of tris(trimethylsilyl)-silan and .alpha...alpha.'-azo-isobutyronitril in organic solvent; and 32-deoxorapamycin in the form of a crystalline solvate.

La présente invention concerne des procédés de production d~une 32-désoxorapamycine à partir d~une 32-iodo- ou 32-hydroxyrapamycine. Dans lesdits procédés, le groupe hydroxy est substitué par le résidu d~un arylthionocarbonate ou d~un arylthiocarbamate, en présence de tris(triméthylsilyl)silane et de .alpha.,.alpha.'-azo-isobutyronitrile, dans un solvant organique. L~invention concerne également de la 32-désoxorapamycine sous forme de solvate cristallin.

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