Process for the preparation of 1-benzyl-4-(5,6-dimethoxy-1-indanon)-2-yl) methyl piperidine hydrochloride (Donepezil HCI)
申请人:——
公开号:US20040158070A1
公开(公告)日:2004-08-12
A process for the preparation of 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl] methyl piperidine hydrochloride (Donepezil HCl) is disclosed. 5,6-Dimethoxy-2-(pyridin-4-yl) methylene inda-1-one is hydrogenated with a noble metal catalyst or a non-oxide derivative of a noble metal catalyst in a solvent at 20-100° C. and 10-90 psi gauge pressure. The resulting 4-[(5,6-dimethoxy-1-indanon)-2-yl] methyl piperidine is alkylated with an alkylating agent in an organic solvent at 20-80° C.
公开了一种制备1-苄基-4-[(5,6-二甲氧基-1-吲哚酮)-2-基]甲基哌啶盐酸盐(多奈哌齐盐酸盐)的方法。在20-100°C和10-90 psi表压下,将5,6-二甲氧基-2-(吡啶-4-基)亚甲基吲哚-1-酮与贵金属催化剂或贵金属催化剂的非氧化物衍生物在溶剂中进行氢化。得到的4-[(5,6-二甲氧基-1-吲哚酮)-2-基]甲基哌啶在有机溶剂中与烷基化试剂进行烷基化反应,反应温度为20-80°C。