PROCESS FOR THE PREPARATION OF URSO-DESOXYCHOLIC ACID FROM 3-ALPHA 7-BETA 12-ALPHA-TRIHYDROXYCHOLANIC ACID

摘要

1. Claims (for the Contracting States : AT, BE, CH, DE, GB, LI, NL) Preparation process of ursodesoxycholic acid with the formula I see diagramm : EP0072293,P9,F2 characterized in that 3 alpha, 7 beta, 12 alpha-trihydroxycholanic acid with the formula II see diagramm : EP0072293,P9,F3 is treated with a reactional derivative of an organic radical with the formula R-CO- in which R represents a hydrogen atom or an alkyl or alkoxy radical having from 1 to 5 carbon atoms or an alkenyloxy radical having from 2 to 5 carbon atoms, a cycloalkyloxy radical having from 3 to 7 carbon atoms or an aralkyloxy radical having from 7 to 12 carbon atoms, an aryl or aralkyl radical having from 6 to 12 carbon atoms, each of these radicals possibly carrying one or more substituents, so as to obtain a product with the formula III : see diagramm : EP0072293,P9,F4 which product with the formula III is treated with bromine in a basic medium so as to obtain a product with the formula IV see diagramm : EP0072293,P9,F5 which product with the formula IV is saponified so as to obtain a product with the formula V : see diagramm : EP0072293,P10,F1 or a salt of this product, which product with the formula V or which salt is treated with hydrazine in the presence of diethylene glycol and a base so as to obtain the sought ursodesoxycholic acid. 1. Claims (for the Contracting State IT) Preparation process of ursodesoxycholic acid with the formula I see diagramm : EP0072293,P10,F2 characterized in that 3 alpha, 7 beta, 12 alpha-trihydroxycholanic acid with the formula II see diagramm : EP0072293,P10,F3 is treated with a reactional derivative of an organic radical with the formula R-CO- in which R represents a hydrogen atom or an alkyl or alkoxy radical having from 1 to 5 carbon atoms or an alkenyloxy radical having from 2 to 5 carbon atoms, a cycloalkyloxy radical having from 3 to 7 carbon atoms or an aralkyloxy radical having from 7 to 12 carbon atoms, an aryl or aralkyl radical having from 6 to 12 carbon atoms, each of these radicals possibly carrying one or more substituents, so as to obtain a product with the formula III : see diagramm : EP0072293,P11,F1 which product with the formula III is treated with an oxidizing agent so as to obtain a product with the formula IV see diagramm : EP0072293,P11,F2 which product with the formula IV is saponified so as to obtain a product with the formula V : see diagramm : EP0072293,P11,F3 or a salt of this product, which product with the formula V or which salt is treated with a reducing agent so as to obtain the sought ursodesoxycholic acid.