| 摘要 |
A method for producing a donepezil hydrochloride which is used as a drug of Alzheimer's disease is provided to massively produce the donepezil hydrochloride through two steps and improve the yield and purity of the donepezil hydrochloride. A method for producing 2-((1-benzylpiperidine-4-yl)methyl -2,3-dihydro-5,6-dimethoxyindene-1-one hydrochloride (donepezil hydrochloride) of the chemical formula 1 comprises: a step of reacting tert-butyl 4-((2-(methoxycarbonyl)-2,3-dihydro-5,6-dimethoxy-1-iodine-1H-indene-2-yl)methyl)piperidine-1-carboxylate of the chemical formula 2 in mixture solution of water and 1-4 carbon under the presence of base; to obtain tert-butyl 4-((2,3-dihydro-5,6-dimethoxy-1-iodine-1H-indene-2-yl)methyl)piperidine-1-carboxylate; and a step of removing N-protection group from the compound of the chemical formula 3 under the presence of organic solvent and acid and reacting benzyl halide under the presence of base to obtain the donepezil hydrochloride.
|
