申请人:John Wyeth & Brother Limited
公开号:US06395902B1
公开(公告)日:2002-05-28
Compounds having the formula
R5O—A—NR4—R2 (V)
where R2 is a heteroaryl group linked to the remainder of the molecule via a carbon atom adjacent a nitrogen atom and R4 and R5 are both hydrogen atoms or together represent —SO— or —SO2— and A is C2-C4 alkylene optionally substituted by one or more lower alkyl groups are novel intermediates in the preparation of pharmaceutically useful piperazine derivatives as end compounds. The compounds having formula V where R4 and R5 are hydrogen may be prepared by a rearrangement of a compound having the formula (VI).
R2O—A—NH2 (VI)
具有R5O—A—NR4—R2 (V)公式的化合物,其中R2是通过相邻氮原子的碳原子与分子的其余部分连接的杂环烷基,而R4和R5都是氢原子,或者一起代表—SO—或—SO2—,而A是C2-C4烷基,可以选择地被一个或多个较低的烷基取代,是制备药用吡嗪基衍生物的新型中间体。具有公式V且R4和R5为氢的化合物可以通过重排具有公式(VI).R2O—A—NH2 (VI)的化合物制备。