A new and efficient enantioselective synthesis of both enantiomers of the calcium channel blocker bepridil
作者:Mohammad Mujahid、Jambu Subramanian、Viswanadh Nalla、Murugesan Sasikumar、Sunita Sharad Kunte、Murugan Muthukrishnan
DOI:10.1039/c6nj02928k
日期:——
enantioselective synthesis of both enantiomers of bepridil, a calcium channel blocker, is reported. Jacobsen's hydrolytic kinetic resolution method was utilized to resolve racemic 2-(isobutoxymethyl)oxirane. The incorporation of the succinimide moiety by the Mitsunobu reaction, which was investigated in detail, occurred without any loss of enantioselectivity. Using this strategy, both enantiomers of the target
据报道,贝普地尔的两种对映体(钙通道阻滞剂)的简洁高效的对映选择性合成。雅各布森的水解动力学拆分方法用于解决外消旋的2-(异丁氧基甲基)环氧乙烷。通过Mitsunobu反应并入琥珀酰亚胺部分,对此进行了详细研究,对映选择性没有任何损失。使用这种策略,可以以高收率和高对映体纯度(ee> 99%)获得目标分子的两种对映体。