Varespladib (1), was synthesized from 4-benzyloxy-1H-indole (2) via acylation with benzenesulfonyl chloride, acetylation, reduction to give 4-benzyloxy-2-ethyl-1H-indole (6), which was subjected to substitution with benzyl bromide, deprotection, esterification, substitution with oxalyl chloride, ammonolysis and hydrolysis with overall yield of 24.8％and the purity of 99.5％.The target compound was characterized by 1H NMR and MS.%以4-苄氧基吲哚 (2) 为原料, 经苯磺酰基保护后, 在吲哚2位引入乙酰基, 经四氢锂铝和三乙基硅氢两步还原将乙酰基还原为乙基, 得4-苄氧基-2-乙基-1H-吲哚 (6), 再引入N-苄基, 4位脱苄后, 用溴乙酸叔丁酯引入乙酸叔丁酯基, 吲哚3位经草酰氯酰化后再氨解, 最后水解叔丁酯得伐瑞拉迪 (1), 总收率24.8％, 纯度99.5％, 其结构经1H NMR及MS确证.
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