维纳卡兰的合成研究进展

Progresses in Synthesis of Vernakalant

传统的抗心律失常药物疗效较好,但具有致心律失常、器官毒性等副作用.新上市的维纳卡兰是一种新型抗心律失常药物,为选择性心房钠/钾离子通道阻滞剂,研究表明在新近发作的心房颤动急性转复方面的疗效优于胺碘酮,且临床应用前景较好,对其合成路线进行综述.

The traditional antiarrhythmic drug is very efficient, but with arrhythmogenic, organ toxicity and other side effects. Vernakalant is a new antiarrhythmic drug of mixed voltage- and frequency-dependent Na＋ and atria-preferred K＋ channel blockers. Recent clinical studies show that vemakalant under development for the acute conversion of atrial fibrillation to sinus rhythm is better than amiodarone, so it can be expected to have a good prospect for clinical application. In this review,representative synthetic routes employing chemical or biological resolution and catalytic asymmetric reactions are briefly summarized.