- Novel Process for Production of Highly Pure Polymorph (I) Donepezil Hydrochloride
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The present invention provides a novel, industrially realizable and economically preferable process for production of highly pure 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methyl piperidine hydrochloride, i.e., donepezil hydrochloride shown in the following reaction scheme, in Polymorph (I) morphological crystal form. (I) In one of the key steps of the process, during the hydrogenation 5,6-dimethoxy 2-(pyridine-4-yhnethylene)indan-1-one hydrochloride is saturated using Pd carbon to get 4-[(5,6-dimethoxy-1-indanon)-2-yl]-methyl piperidine at more than 97% HPLC purity. In the crystallization step donepezil-hydrochloride is crystallized from an aqueous alcoholic solvent to get Polymorph (I) in at least 99.95% HPLC purity.
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Page/Page column 7-8
(2009/01/20)
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- New synthesis of donepezil through palladium-catalyzed hydrogenation approach
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A new, economical, and efficient process has been developed for large-scale synthesis of donepezil 1, an anti-Alzheimer's drug. The process involves palladium-catalyzed hydrogenation of (2E)-5,6-dimethoxy-2-(pyridin-4- ylmethylene)indan-1-one 6 to provide 5,6-dimethoxy-2-(piperidin-4-ylmethyl) indan-1-one 8 as a key step. Copyright Taylor & Francis LLC.
- Elati, Chandrashekar R.,Kolla, Naveenkumar,Chalamala, Subrahmanyeswara Rao,Vankawala, Pravinchandra J.,Sundaram, Venkataraman,Vurimidi, Himabindu,Mathad, Vijayavitthal T.
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p. 169 - 174
(2007/10/03)
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