左旋盐酸去甲基苯环壬酯的合成新方法

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的贵重原料(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。

Facile synthetic method of levodesmethylphencynonate hydrochloride

Levodesmethylphencynonate hydrochloride（1）,a novel selective M4 muscarine receptor antagonist,has been chosen as a candidate of anti-Parkinson′s disease drug characterized by its good efficiency,high selectivity and low toxicity.A new synthetic method in the search for more economical and environmental friendly process was developed.The starting compound N,N-diethoxylmethy benzyl amine was prepared by benzyl amine and ethanol,then via Mannich reaction with cyclohexanone,afterwards selective hydrogenation and ester exchange with（R）-methyl-α-phenyl-α-cyclopentyl-α-hydroxy acid ester,hydrogenation,saltization to obtain target compound（1）.The overall yield was 8.0%,which increased 10.6% based on common chiral raw material（R）-methyl-α-phenyl-α-cyclopentyl-α-hydroxy acid ester.The chemical structure of levodesmethylphencynonate hydrochloride was characterized by MS,1H-NMR and element analysis.Compared with the original synthetic process,the new route is facile and suitable for industrialized production with lower cost,lower pollution and higher yield.