发明名称 PROCESSES FOR PREPARING RIVAROXABAN
摘要 Processes and intermediates for preparing rivaroxaban, and analogs and derivatives thereof, and pharmaceutically acceptable salts of each of the foregoing, are described herein.
申请公布号 US2015175590(A1) 申请公布日期 2015.06.25
申请号 US201314390527 申请日期 2013.04.04
申请人 INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATION 发明人 McCarthy James R.
分类号 C07D413/14;C07D303/36;C07D301/02 主分类号 C07D413/14
代理机构 代理人
主权项 1. A process for preparing rivaroxaban or a pharmaceutically acceptable salt thereof, the process comprising one or more steps selected from the group consisting of (a) mixing a compound of formula (A)or a salt thereof, with an acylating agent to prepare a compound of formula (B) (b) crystallizing the compound of formula (B); (c) mixing the compound of formula (B) with a compound of formula (C)to prepare a compound of formula (D)or a salt thereof; where RA is halo or a protected amino group; and RB is halo, amino or a salt thereof, or a protected amino group; (d) crystallizing the compound of formula (D); (e) converting the compound of formula (D) or a salt thereof, where RB is halo, or a protected amino group, into a compound of formula (E)or a salt thereof; (f) converting the compound of formula (D) or a salt thereof, where RB is halo, or a protected amino group, into a compound of formula (F) (g) reducing the compound of formula (F) or a salt thereof, into a compound of formula (E) (h) mixing the compound of formula (E) or a salt thereof with an acylating agent to prepare rivaroxaban, or a salt thereof; and (i) crystallizing rivaroxaban or a salt thereof from an organic acid; and combinations thereof.
地址 Indianapolis IN US