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以N-苄基苯胺为原料,经亲核取代、酯胺交换和氨基取代3步反应得到依福地平关键中间体3-氨基-2-丁烯酸-2-(N-苄基-N-苯基)氨基乙酯(氨基片段)。酯交换一步采用碱性催化剂替代原工艺中酸性催化剂;氨基取代一步添加ZSM-5分子筛催化,并采用不锈钢曝气头取代原工艺中导气管。新工艺缩短了反应的时间,降低了氨气的用量,提高了反应收率。改进后的工艺,总收率提高至72.4%,较原工艺提高了9.0%,生产成本降低,操作简便易行,适合工业化生产。
Using N-benzyl aniline as starting material, 3-amino-2-butenoic acid 2- (N-benzyl-N- Phenyl) aminoethyl (amino fragment). In the transesterification step, a basic catalyst was used to replace the acidic catalyst in the original process. Amino substitution was added to the ZSM-5 molecular sieve for catalysis, and a stainless steel aeration head was used to replace the air pipe in the original process. The new process shortens the reaction time, reduces the amount of ammonia, and improves the reaction yield. The improved process, the total yield increased to 72.4%, compared with the original process increased by 9.0%, lower production costs, easy to operate, suitable for industrial production.