Banitt E H, Schmid J R, Newmark R A
J Med Chem. 1986 Feb;29(2):299-302. doi: 10.1021/jm00152a021.
The antiarrhythmic agent flecainide acetate was resolved by fractional crystallization of its diastereomeric alpha-bromocamphor-pi-sulfonate salts. Optical purity of the two enantiomers was shown to be greater than 99% by an NMR technique using the chiral shift reagent Eu(hfbc)3. Antiarrhythmic effects of flecainide and its enantiomers were assessed in two different animal models, chloroform-induced ventricular fibrillation in mice and ouabain-induced ventricular tachycardia in dogs. The two enantiomers were highly effective in suppressing both of these experimental arrhythmias and appeared to be essentially equipotent. No significant differences were found either between the two enantiomers or between the enantiomers and racemic flecainide.
抗心律失常药醋酸氟卡尼通过其非对映体α-溴樟脑-π-磺酸盐的分步结晶进行拆分。使用手性位移试剂Eu(hfbc)3的核磁共振技术表明，两种对映体的光学纯度均大于99%。在两种不同的动物模型中评估了氟卡尼及其对映体的抗心律失常作用，即氯仿诱导的小鼠心室颤动和哇巴因诱导的犬室性心动过速。两种对映体在抑制这两种实验性心律失常方面都非常有效，并且似乎基本等效。在两种对映体之间以及对映体与外消旋氟卡尼之间均未发现显著差异。
