发明名称 NEW PROCESS FOR THE PRODUCTION OF TIOTROPIUM SALTS
摘要 The invention relates to a new process for preparing tiotropium salts of general formula 1;;wherein X− may have the meanings given in the claims and in the specification.
申请公布号 US2015225395(A1) 申请公布日期 2015.08.13
申请号 US201514694155 申请日期 2015.04.23
申请人 Boehringer Ingelheim Pharma GmbH & Co. KG 发明人 BRANDENBURG Joerg;PFRENGLE Waldemar
分类号 C07D451/10 主分类号 C07D451/10
代理机构 代理人
主权项 1. A process for preparing tiotropium salts of formula 1wherein X− represents bromide,comprising: reacting in one step a compound of formula 2wherein Y− is hexafluorophosphate, with a compound of formula 3wherein R is methoxy or ethoxy, in a solvent selected from acetone, acetonitrile or pyridine with the addition of a catalyst selected from zeolites to obtain a compound of formula 4wherein the group Y− has the meaning given above, and without being isolated, the compound of formula 4 is converted into the compound of formula 1 by reacting formula 4 with a salt cat+X−, wherein cat+denotes a cation selected from the group consisting of Li+, Na+, and K+, and X− has the meaning given above.
地址 Ingelheim am Rhein DE