发明名称 SYNTHESIS METHOD AND INTERMEDIATES USEFUL IN THE PREPARATION OF PYRROLOBENZODIAZEPINES
摘要 A compound of formula I wherein: R7 is selected from: ORA, where RA is selected from C1-4 saturated alkyl, optionally substituted by phenyl, which may bear a chloro substituent, pyridyl and furanyl; chloro; NH2; —CH2—O—C(═O)Me; R8 is OProto, where Proto is a silicon-based oxygen protecting group orthogonal to Rc; R9 is selected from H, methyl and methoxy; Rs is selected from CF3, (CF2)3CF3, CH3 and (formula 2) and Rc is selected from: (i) C(═O)—ORC1, where RC1 is a saturated C1-4 alkyl group; (ii) —CH2—O—C(═O)RC2, where RC2 is methyl or phenyl; (iii) CH2—O—Si—(RSi1)(RSi2)(RSi3), where RSi1, RSi2, RSi3 are independently selected from C1-6 a saturated alkyl group and a phenyl group; and (iv) C(—YRC3)(—YRC4) where each Y is independently O or S, and where RC3 and RC4 are independently a saturated C1-4 alkyl group, or together form a C2-3 alkylene.
申请公布号 EP2751076(A1) 申请公布日期 2014.07.09
申请号 EP20120772781 申请日期 2012.10.12
申请人 SPIROGEN SÀRL 发明人 HOWARD, PHILIP WILSON;TIBERGHIEN, ARNAUD
分类号 C07D207/20;A61K31/5517;A61P35/00;C07D207/24;C07D207/27;C07D401/12;C07D409/12;C07D413/12;C07D487/04;C07D519/00 主分类号 C07D207/20
代理机构 代理人
主权项
地址