A new efficient method for conversion of corticosteroid 17.ALPHA.,21-cyclic ortho esters to 17.ALPHA.-acyloxy-21-chloro-21-deoxy derivatives.

1 January 1983

journal article
research article
Published by Pharmaceutical Society of Japan in CHEMICAL & PHARMACEUTICAL BULLETIN

Vol. 31 (1) , 12-19
https://doi.org/10.1248/cpb.31.12

Abstract

The reaction of corticosteroid 17.alpha.,21-cyclic ortho esters with various chloroformates afforded the corresponding 17.alpha.-acyloxy-21-chloro-21-deoxy derivatives in good yields. Several new derivatives, 17.alpha.-acyloxy-21-chloro-11.beta.-hydroxy-6.alpha.-methyl-1,4-pregnadiene-3,20-diones, exhibited potent vasoconstrictive activities.

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