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对硝基苯甲酰 -β-丙氨酸 (1 )是合成抗结肠炎药物巴柳氮的中间体。文献 [1]报道的合成方法是 :β-丙氨酸 (3)先成盐 ,在水溶液中与对硝基苯甲酰氯 (2 )低温反应 ,再用冰 - HCl混合液酸化 ,收率为 79.1 %。作者改用相转移催化 ,以 TEBA为相转移催化剂 ,常温反应 ,1的收率提高到
Nitrobenzoyl-β-alanine (1) is an intermediate for the synthesis of balsalazide, an anti-colitis drug. The synthetic method reported in [1] is as follows: β-alanine (3) is first salified and reacted with p-nitrobenzoyl chloride (2) at low temperature in aqueous solution and then acidified with ice- 79.1%. The author used phase transfer catalysis to TEBA phase transfer catalyst, room temperature reaction, a yield of 1 to