Synthesis of 3‐arylsulfonylmethyl‐1,2,4‐oxadiazole‐5‐carboxylic acid derivatives

Abstract
Several new 3‐arylsulfonylmethyl‐1,2,4‐oxadiazole‐5‐carboxylic acid derivatives have been synthesized. A typical example, 3‐[(4‐chlorophenylsulfonyl)methyl]‐1,2,4‐oxadiazole‐5‐carboxylic acid ethyl ester (2c), was prepared from the reaction of 2‐(4‐chlorophenylsulfonyl)acetamide oxime (1c) with ethyl oxalyl chloride. The hydrazide derivative (3f) showed antihypertensive activity in rats. Various structural modifications to improve activity are discussed.

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