Stereoselective transacetalization of steroidal c-22 acetonide

Details Stereoselective transacetalization of steroidal c-22 acetonide Stereoselective transacetalization of steroidal c-22 acetonide

C - Chemistry, Metallurgy

07

J

C07J 71/00 (2006.01) C07J 75/00 (2006.01)

Patent

CA 2459880

The present invention is a process for the preparation of rofleponide of formula (II) where the 22R/22S ratio is 90/10 or greater which comprises contacting an acetonide of formula (I) with CH3-CH2-CH2-CHO (III) in the presence of perchloric acid where the concentration of the acetonide (I) is from about 1 g/20 ml to about 1 g/50 ml in the absence of an inert material.

L'invention concerne un procédé de préparation de rofléponide de formule (II) présentant un rapport 22R/22S supérieur ou égal à 90/10. Ce procédé comprend l'étape consistant à mettre un acétonide de formule (I) au contact du composé CH¿3?-CH¿2?-CH¿2?-CHO (III), en présence d'acide perchlorique, la concentration en acétonide (I) étant comprise entre environ 1 g/20 ml et environ 1 g/50 ml en l'absence d'une matière inerte.

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