Liu Lin
2007
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Chemical Reagents
Abstract
3-Methylaminopiperidine,an intermediate for the manufacture of Balofloxacin,was synthesized from nicotinic amide in four steps.The Hofmann reaction of nicotinic amide gave 3-aminopyridine in 85% yield.Treatment of 3-aminopyridine with AFA at room temperature led to the formation of 3-formamidopyridine in 95% yield.3-Methylaminopyridine was then prepared in 95% yield via the reduction of 3-formamidopyridine with LiAlH4.The final product 3-methylaminopiperidine dihydrochloride was then obtained in 92% yield by further reduction of 3-methylaminopyridine with Na in ethyl alcohol.The structures of the final product and the intermediates were characterized by 1HNMR.Purity of the final product was analyzed by HPLC.