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目的优化人精子顶体酶抑制剂4-胍基苯甲酸-4′-乙酰氨基苯基酯盐酸盐(AGB)的合成工艺。方法按L9(34)正交表设计考察了缩合剂(A)、反应时间(B)和溶剂(C)3个主要因素对关键中间体4-胍基苯甲酸盐酸盐(3)与4-乙酰氨基苯酚缩合反应制备AGB收率的影响。结果缩合反应合成AGB的最优反应条件为C2B1A2,收率从44%提高到70%。结论新工艺反应条件温和、后处理简便、收率较高。
Objective To optimize the synthetic process of 4-guanidinobenzoate-4’-acetamidophenyl ester hydrochloride (AGB), a human sperm acrosin inhibitor. Methods According to the orthogonal design of L9 (34), the effect of the three main factors of condensing agent (A), reaction time (B) and solvent (C) on the reaction of 4-guanidinobenzoic acid hydrochloride Effect of 4-Acetaminophenol Condensation on the Yield of AGB. Results The optimal reaction conditions for the synthesis of AGB by condensation reaction were C2B1A2. The yield increased from 44% to 70%. Conclusion The new process mild reaction conditions, post-processing simple, high yield.