The present invention provides a production method of heterocyclic compound having an excellent CH24H inhibitory action, which is suitable for industrial production.
In the present invention, a 2-halogenonicotinic acid or a reactive derivative thereof or a salt thereof is reacted with 4-benzyl-4-hydroxypiperidine acid addition salt to give a (4-benzyl-4-hydroxypiperidin-1-yl) (2-halogenopyridin-3-yl)methanone or a salt thereof, and then the obtained compound is reacted with pyridine-4-boronic acid or a reactive derivative thereof or a salt thereof in the presence of a metal catalyst and a base to give (4-benzyl-4-hydroxypiperidin-1-yl) (2,4′-bipyridin-3-yl)methanone or a salt thereof.
本发明提供了一种具有优异的 CH24H 抑制作用的
杂环化合物的生产方法,该方法适用于工业生产。
在本发明中,2-卤代
烟酸或其活性衍
生物或其盐与
4-苄基-4-羟基哌啶酸加成盐反应,得到(
4-苄基-4-羟基哌啶-1-基)(2-卤代
吡啶-3-基)甲酮或其盐、然后在
金属催化剂和碱存在下,将得到的化合物与
吡啶-4-
硼酸或其活性衍
生物或其盐反应,得到(
4-苄基-4-羟基哌啶-1-基)(2,4′-联
吡啶-3-基)甲酮或其盐。