STEREOSELECTIVE TRANSACETALIZATION OF STEROIDAL C-22 ACETONIDE

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...

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Bibliographic Details
Main Authors REEDER, LISA, M, STANCHINA, COREY, L
Format Patent
LanguageEnglish
French
Published 03.04.2003
Edition7
Subjects
CHEMISTRY
METALLURGY
ORGANIC CHEMISTRY
STEROIDS
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Summary: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 CH3-CH2-CH2-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.
Bibliography:Application Number: WO2002US28124