QUINOLYL PYRROLO PYRIMIDYL CONDENSED-RING COMPOUND AND SALT THEREOF
申请人:Taiho Pharmaceutical Co., Ltd.
公开号:US20140057899A1
公开(公告)日:2014-02-27
The present invention provides a new compound that has an inhibitory action against EGFR and that has cell growth inhibitory effects. The present invention further provides a pharmaceutical preparation useful for preventing and/or treating cancer, based on the EGFR inhibitory effect of the compound. A compound represented by the following Formula (I)
or a salt thereof.
RCM+AD=T2: In the presence of the C16‐methylene group, regioselective ring‐closing metathesis (RCM) formed the (12E)‐endocyclic double bond, which underwent Os‐catalyzed asymmetric dihydroxylation (AD) to give the desired 12,13‐diol intermediate required for the totalsynthesis of amphidinolideT2 in 16 linear steps in 8.0 % overall yield.
RCM + AD = T2:在存在C16-亚甲基的情况下,区域选择性闭环复分解(RCM)形成了(12 E)-环内双键,该双键经过Os催化的不对称二羟基化(AD)得到所需的12以16个线性步骤全合成Amphidinolide T2所需的,13-二醇中间体,总收率为8.0%。