PROCESS FOR THE PREPARATION OF INTERMEDIATES IN THE SYNTHESIS OF VITAMIN-D3 METABOLITES, AND INTERMEDIATES

The present disclosure is directed to a process and intermediates for the synthesis of Vitamin D3 metabolites such as 1,25-dihydroxycholecalciferol, 25-hydroxycholecalciferol and 24R,25-dihydroxycholecalciferol from 17-keto steroids via intermediates having the natural steroid configuration at the 2...

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Bibliographic Details
Main Authors BATCHO, ANDREW D, USKOKOVIC, MILAN R, BERGER, DONALD E. JR
Format Patent
LanguageEnglish
German
Published 18.08.1982
Subjects
CHEMISTRY
METALLURGY
ORGANIC CHEMISTRY
STEROIDS
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Summary:The present disclosure is directed to a process and intermediates for the synthesis of Vitamin D3 metabolites such as 1,25-dihydroxycholecalciferol, 25-hydroxycholecalciferol and 24R,25-dihydroxycholecalciferol from 17-keto steroids via intermediates having the natural steroid configuration at the 20-position. These novel intermediates are prepared from 17-keto steroids by reaction with ethyltriphenylphosphonium halides followed by reaction with formaldehyde to form comounds having the natural steroid configuration at the 20-position and which are suitable substrates for the preparation of the aforementioned Vitamin D3 metabolites.
Bibliography:Application Number: EP19810108386