首页 | 本学科首页   官方微博 | 高级检索  
     检索      


An improved synthesis of butyl 4-[(4-amino-5-chloro-2-methoxybenzoyl)amino]-1-piperidineacetate (AU-224).
Authors:J Sakaguchi  T Higashi  T Azuma  T Suzuki  N Iwasaki  N Kondo  O Nagata  H Kato  M Hanaoka
Institution:Research Division, Hokuriku Seiyaku Co., Ltd., Katsuyama, Fukui, Japan. jun.sakaguchi@hokuriku-seiyaku.co.jp
Abstract:A new and facile route for the synthesis of the novel gastrointestinal prokinetic butyl 4-(4-amino-5-chloro-2-methoxybenzoyl)amino]-1-piperidineacetate (1b), which exhibited potent gastro- and colon-prokinetic activities by oral administration without significant side effects, was established. The key intermediate, butyl 4-amino-1-piperidineacetate (16), was prepared from commercially available 4-amino-1-benzylpiperidine (2) in a high yield with four steps. Compound 1b was prepared by condensation of commercially available 4-amino-5-choloro-2-methoxybenzoic acid (7) with 16 in 84% yield. This improved synthetic route was appropriate for large-scale synthesis of 1b.
Keywords:
设为首页 | 免责声明 | 关于勤云 | 加入收藏

Copyright©北京勤云科技发展有限公司  京ICP备09084417号