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 ...
