Shen Li
2012
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Journal
Chinese Journal of Pharmaceuticals
Abstract
2-Chloro-4-(piperidin-1-ylmethyl)pyridine,the intermediate of lafutidine,was synthesized from 2-amino-4-methylpyridine by successive chlorination with CuCl/HCl and sulfuryl chloride to give 2-chloro-4-(chloromethyl)pyridine,followed by condensation with piperidine in DMF with an overall yield of about 62%.