专利号:US-2014128613-A1 优先权日:2011-03-25 标 题:A process for preparation of intermediates of donepezil hydrochloride 发明人:GURUSAMY RENUGADEVI; ROY MITA; SHANMUGANATHAN RAMASUBRAMANIAN; JAGTAP ASHUTOSH; HARIHARAN SIVARAMAKRISHNAN; MISHRA SUSHIL KUMAR; WANKHEDE KARUNA 权利人:GURUSAMY RENUGADEVI; ROY MITA; SHANMUGANATHAN RAMASUBRAMANIAN; JAGTAP ASHUTOSH; HARIHARAN SIVARAMAKRISHNAN; MISHRA SUSHIL KUMAR; WANKHEDE KARUNA; PIRAMAL ENTPR LTD 摘要:The present invention provides a process for the preparation of key intermediate for the synthesis 5,6-dimethoxy-2-[[1-(phenylmethyl)-4-piperidinyl]methyl]-1-indanone hydrochloride (donepezil hydrochloride). The present invention particularly provides a process for the preparation of 5,6-dimethoxy-2-(4-pyridylmethylene)-1-indanone comprising condensation of 5,6-dimethoxy-1-indanone with 4-pyridinecarboxaldehyde using an alkali metal hydroxide as a mild base in the presence of demineralized water as a solvent at a temperature in the range of 15° C. to 45° C. to yield 5,6-dimethoxy-2-(4-pyridylmethylene)-1-indanone, which is subsequently benzylated using benzyl bromide in the presence of solvent at a reflux temperature to yield 1-benzyl-4-[(5,6-dimethoxy-1-indanone-2-yl)methylene]pyridinium bromide.
参考文献:10.1107/s1600536810039486 摘要:Ali MA, Ismail R, Tan SC, Yeap CS, Fun HK. (E)-5,6-Dimeth-oxy-2-(pyridin-4-yl-methyl-idene)-2,3-dihydro-1H-inden-1-one. Acta Crystallogr Sect E Struct Rep Online. 2010 Oct 09;66(Pt 11):o2753.