Process for the production of 17-esters of clobetasol

C - Chemistry – Metallurgy – 07 – J

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260/14, 260/83

C07J 7/00 (2006.01) C07J 71/00 (2006.01)

Patent

CA 1220468

- 1 - PROCESS FOR THE PRODUCTION OF 17-ESTERS OF CLOBETASOL ABSTRACT This invention relates to an improved process for the preparation of 17-esters of Clobetasol having the formula Image II which consists in treatment of 9.beta.,11.beta.-epoxy-16.beta.-methyl- pregna-1,4-diene-17,21-diol-3,20-dione 17-esters with mesyl chloride to give the corresponding 21-chloro-deriv- ative, followed by opening of the epoxide grouping with hydrogen fluoride. The invention also relates to new 17-esters of 21-chloro-9.beta.,11.beta.-epoxy-17-hydroxy-16.beta.-methyl- pregna-1,4-diene-3,20-dione, useful as intermediates for the preparation of therapeutically active 9.alpha.-halo-11.beta.- hydroxy derivatives.

445603

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