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目的合成新型M4受体选择性拮抗剂左旋盐酸去甲基苯环壬酯。方法以苄胺为原料制备N,N-二乙氧基甲基苄胺,该苄胺与环己酮反应、选择性还原,再与(R)-α-苯基-α-环戊基-α-羟基乙酸甲酯反应,经氢化、成盐得到目标产物左旋盐酸去甲基苯环壬酯,总收率为8.0%。结果与结论目标化合物的结构经元素分析、核磁共振氢谱、质谱确证。新方法操作简便,以新旧合成路线中共有贵重原料(R)-α-苯基-α-环戊基-α-羟基乙酸甲酯计算,产品收率较原方法提高了10.6%,降低了成本,且利于环保。
OBJECTIVE: To synthesize nor-phencyclononanilate, a new M4 selective receptor antagonist. Methods N, N-diethoxymethylbenzylamine was prepared from benzylamine by reaction with cyclohexanone and selective reduction, and then reacted with (R) -α-phenyl-α-cyclopentyl- α-hydroxyacetic acid methyl ester. Hydrogenation and salt formation gave the target product decyclononanisole hydrochloride in a total yield of 8.0%. Results and Conclusion The structure of the target compound was confirmed by elemental analysis, 1H-NMR and MS. The new method is simple and easy to operate. Based on the raw materials (R) -α-phenyl-α-cyclopentyl-α-hydroxymethyl acetate shared by both old and new synthetic routes, the yield of the product is increased by 10.6% , And conducive to environmental protection.