盐酸替利定的合成

Synthesis of Tilidine Hydrochloride

苯乙酸乙酯经亲核加成、脱羧制得α-亚甲基苯乙酸乙酯(4):另以巴豆醛与二甲胺在THF中反应制得1,3-二(二甲胺基)-1-丁烯(6)。4与6经缩合、分离、成盐制得盐酸替利定,总收率约15%(以苯乙酸乙酯计)。

Tilidine hydrochloride was synthesized from ethyl 2-phenylacetate by nucleophilic addition and decarboxylation to give ethyl α-methylenephenylacetate （4）, which was subjected to condensation with 1,3-di- （dimethylamino）- 1-butene （6）, followed by separation and salt formation with an overall yield of about 15 % （based on ethyl 2-phenylacetate）. Compound 6 was prepared from 2-butenal by reaction with dimetaglamine.