Synthesis and evaluation of antiinflammatory activities of a series of corticosteroid 17. alpha.-esters containing a functional group

H Ueno, A Maruyama, M Miyake, E Nakao…

Index: Ueno; Maruyama; Miyake; Nakao; Umezu; Nitta Journal of Medicinal Chemistry, 1991 , vol. 34, # 8 p. 2468 - 2473

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Citation Number: 47

Abstract

A series of 21-desoxy-21-chlorocorticosteroids that contain a functionalized ester group at 17a has been prepared and examined to separate their systemic activity from topical antiinflammatory activity. Introduction of the functionalized ester group at 17a was carried out by an acid-catalyzed formation of cyclic ortho esters with 17a, 21-hydroxyl groups of corticosteroids and subsequent acid-catalyzed hydrolysis. As for the functional group, ...