Total synthesis of SR 121463 A, a highly potent and selective vasopressin V2 receptor antagonist

…, MC Davis, Y Altas, JP Snyder, DC Liotta

Index: Venkatesan; Davis; Altas; Snyder; Liotta Journal of Organic Chemistry, 2001 , vol. 66, # 11 p. 3653 - 3661

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Citation Number: 93

Abstract

SR 121463 A, 1, is a promising nonpeptide prototype for potent and selective antagonism of the vasopressin V2 receptor subtype and, thus, a candidate for control of the clinically debilitating condition of hyponatremia and its associated syndromes. In the present work, we present a novel and stereoselective synthesis that stems from the preparation of three key intermediates: the substituted benzenesulfonyl chloride 2, the N-protected oxindole 3, and ...