发明名称 Process for the preparation of compounds useful as inhibitors of SGLT2
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 US9174971(B2) 申请公布日期 2015.11.03
申请号 US201012904233 申请日期 2010.10.14
申请人 Janssen Pharmaceutica NV 发明人 Farina Vittorio;Lemaire Sebastien François Emmanuel;Houpis Ioannis N.
分类号 C07D309/10;C07D409/14;C07D409/10;C07F3/06 主分类号 C07D309/10
代理机构 代理人
主权项 1. A process for the preparation of compounds of formula (I) wherein Ring A and Ring B are one of the following: (1) Ring A is an optionally substituted unsaturated monocyclic heterocyclic ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring; or (2) Ring A is an optionally substituted benzene ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring, or an optionally substituted unsaturated fused heterobicyclic ring wherein Y is linked to the heterocyclic ring of the fused heterobicyclic ring; or (3) Ring A is an optionally substituted unsaturated fused heterobicyclic ring, wherein the sugar moiety X-(sugar) and the moiety —Y-(Ring B) are both on the same heterocyclic ring of the fused heterobicyclic ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring; X is a carbon atom; Y is —(CH2)n—; wherein n is 1 or 2; provided that in Ring A, X is part of an unsaturated bond; or a pharmaceutically acceptable salt or solvate thereof; comprising reacting a compound of formula (VII), wherein M2 is a zinc species, with a compound of formula (VIII), wherein each Z is pivaloyl and wherein LG2 is bromo; in a mixture of an ether solvent and a hydrocarbon solvent; wherein the ether solvent is selected from the group consisting of di-n-butyl ether and cyclopentylmethyl ether; at a temperature in the range of from about 60° C. to about 95° C.; to yield the corresponding compound of formula (IX); de-protecting the compound of formula (IX); to yield the corresponding compound of formula (I).
地址 Beerse BE