发明名称 PROCESS FOR THE PREPARATION OF COMPOUNDS USEFUL AS INHIBITORS OF SGLT-2
摘要 The present invention is directed to a novel process for the preparation of compounds having inhibitory activity against sodium-dependent glucose transporter (SGLT) being present in the intestine or kidney.
申请公布号 US2014206859(A1) 申请公布日期 2014.07.24
申请号 US201214118653 申请日期 2012.05.18
申请人 Wells Kenneth M.;Li Xun;Branum Shawn;Nomura Sumihiro;Matsumura Yosuke 发明人 Wells Kenneth M.;Li Xun;Branum Shawn;Nomura Sumihiro;Matsumura Yosuke
分类号 C07H19/044 主分类号 C07H19/044
代理机构 代理人
主权项 1. A process for the preparation of a compound of formula (I-T) or a pharmaceutically acceptable salt or prodrug thereof; comprising reacting a compound of formula (V-T), wherein PG1 is an oxygen protecting group with a compound of formula (VII-T), wherein A1 is an acyl halide; in the presence of a first Lewis acid; in a first organic solvent; to yield the corresponding compound of formula (X-T); reacting the compound of formula (X-T) with a reducing system; in the presence of an alcohol of formula A2OH, wherein A2 is methyl, ethyl or isopropyl; in a second organic solvent; to yield the corresponding compound of formula (XI-T); reacting the compound of formula (XI-T) with a reducing agent; in the presence of a second Lewis acid; in a third organic solvent; to yield the corresponding compound of formula (IX-T); de-protecting the compound of formula (IX-T); to yield the corresponding compound of formula (I-T).
地址 Doylestown PA US