发明名称 Process for the preparation of chiral 8-(3-aminopiperidin-1-yl)-xanthines
摘要 The invention relates to an improved process for preparing enantiomerically pure 8-(3-aminopiperidin-1-yl)-xanthines.
申请公布号 US8883805(B2) 申请公布日期 2014.11.11
申请号 US201313782149 申请日期 2013.03.01
申请人 Boehringer Ingelheim International GmbH 发明人 Pfrengle Waldemar;Pachur Thorsten;Nicola Thomas;Duran Adil
分类号 C07D473/04;C07D473/06 主分类号 C07D473/04
代理机构 代理人 Morris Michael P.;Kershner David L.
主权项 1. A compound of formula (II) or an enantiomer thereof, wherein R1 is a phenylcarbonylmethyl, benzyl, naphthylmethyl, pyridinylmethyl, pyrimidinyl-methyl, quinolinylmethyl, isoquinolinylmethyl, quinazolinylmethyl, quinoxalinylmethyl, naphthyridinylmethyl or phenanthridinylmethyl group wherein the aromatic or heteroaromatic moiety is in each case mono- or disubstituted by Ra, where the substituents may be the same or different and Ra is a hydrogen, fluorine, chlorine or bromine atom or a cyano, methyl, trifluoromethyl, ethyl, phenyl, methoxy, difluoromethoxy, trifluoromethoxy or ethoxy group,or two Ra radicals, when they are bonded to adjacent carbon atoms, may also be an —O—CH2—O— or —O—CH2—CH2—O— group, R2 is a methyl, ethyl, propyl, isopropyl, cyclopropyl or phenyl group, and R3 is a 2-buten-1-yl, 3-methyl-2-buten-1-yl, 2-butyn-1-yl, 2-fluorobenzyl, 2-chlorobenzyl, 2-bromobenzyl, 2-iodobenzyl, 2-methylbenzyl, 2-(trifluoromethyl)benzyl or 2-cyanobenzyl group.
地址 Ingelheim am Rhein DE