PROCESS FOR PRODUCTION OF 4-(5-METHYLPYRIDIN-2-YLAMINO)PIPERIDINE-1-CARBOXYLIC ACID DERIVATIVES
申请人:Kyorin Pharmaceutical Co., Ltd.
公开号:EP2476677A1
公开(公告)日:2012-07-18
A novel method for manufacturing 5-methyl-2-(piperidin-4-ylamino)pyridine is established. This method can be used as an industrial manufacturing method to produce a 4-(5-methylpyridin-2-ylamino)piperidine-1-carboxylic acid derivative represented by the general formula,
(wherein R represents a linear or branched alkyl group having 1 to 6 carbon atoms or an aralkyl group having 7 to 12 carbon atoms)
in a reaction solution having an aromatic monocyclic hydrocarbon as a reaction medium, in the presence of sodium triacetoxyborohydride as a reducing agent, or after adding sodium borohydride and acetic acid to the reaction solution in advance.
建立了一种制造 5-甲基-2-(哌啶-4-基氨基)吡啶的新方法。该方法可作为一种工业制造方法,用于生产通式为 4-(5-甲基吡啶-2-基氨基)哌啶-1-羧酸衍生物、
(其中 R 代表具有 1 至 6 个碳原子的直链或支链烷基或具有 7 至 12 个碳原子的芳烷基)。
在以芳香族单环烃为反应介质的反应溶液中,以三乙酰氧基硼氢化钠为还原剂,或预先在反应溶液中加入硼氢化钠和乙酸。