发明名称 PROCESSES FOR PREPARING OF GLUCOPYRANOSYL-SUBSTITUTED BENZYL-BENZENE DERIVATIVES AND INTERMEDIATES THEREIN
摘要 The present invention relates to processes for preparing the compounds of general formula I,;;wherein the groups R1 and R3 are defined according to claim 1. Furthermore this inventions relates to intermediates obtained in these processes.
申请公布号 US2015322053(A1) 申请公布日期 2015.11.12
申请号 US201514805838 申请日期 2015.07.22
申请人 Boehringer Ingelheim International GmbH 发明人 ECKHARDT Matthias;HIMMELSBACH Frank;WANG Xiao-Jun;TANG Wenjun;SUN Xiufeng;ZHANG Li;KRISHNAMURTHY Dhileepkumar;SENANAYAKE Christopher Hugh;HAN Zhengxu
分类号 C07D407/12;C07D309/10;C07F3/02;C07H19/01;C07H15/04;C07F1/02 主分类号 C07D407/12
代理机构 代理人
主权项 1. Process for preparing the compounds of general formula I, wherein R1 denotes cyclobutyl, cyclopentyl, cyclohexyl, R-tetrahydrofuran-3-yl, S-tetrahydrofuran-3-yl or tetrahydropyran-4-yl; and R3 denotes hydrogen; said method comprised of the steps of cleaving a compound of general formula II wherein R1 is defined as hereinbefore and R2 independently of one another denote hydrogen, (C1-18-alkyl)carbonyl, (C1-18-alkyl)oxycarbonyl, arylcarbonyl, aryl-(C1-3-alkyl)-carbonyl, aryl-C1-3-alkyl, allyl, RaRbRcSi, CRaRbORc, wherein two adjacent groups R2 may be linked with each other to form a bridging group SiRaRb, CRaRb or CRaORb—CRaORb; with the proviso that at least one substituent R2 is not hydrogen; Ra, Rb, Rc independently of one another denote C1-4-alkyl, aryl or aryl-C1-3-alkyl, while the alkyl groups may be mono- or polysubstituted by halogen; L1 independently of one another are selected from among fluorine, chlorine, bromine, C1-3-alkyl, C1-4-alkoxy and nitro; while by the aryl groups mentioned in the definition of the above groups are meant phenyl or naphthyl groups, which may be mono- or polysubstituted with L1; the protective groups R2 not being hydrogen are cleaved.
地址 Ingelheim am Rhein DE