efficient palladium-catalyzed nucleomethylation of alkynes for the simultaneous construction of the heteroaromatic ring and methyl group. The 3-methylindoles, 3-methylbenzofurans and 4-methylisoquinolines were obtained in moderate to excellent yields. Notably, this methodology was employed as a key step for synthesis of a pregnane X receptor antagonist, zindoxifene, bazedoxifene and AFN-1252. The kinetic studies
在此,我们公开了一种新颖且有效的
钯催化
炔烃核甲基化,用于同时构建杂芳环和甲基。
3-甲基吲哚、
3-甲基苯并呋喃和
4-甲基异喹啉以中等至优异的产率获得。值得注意的是,该方法被用作合成孕烷 X 受体拮抗剂、津多昔芬、
巴多昔芬和 AFN-1252 的关键步骤。动力学研究表明,还原消除可能是决定速率的步骤。