Knorr H, Reichl R, Traunecker W, Knappen F, Brandt K
Arzneimittelforschung. 1984;34(12):1709-13.
The enantiomers of etilefrine (Effortil) were produced by enantioselective hydrogenation. The optical purity was determined by conversion with (+)-[(R)-tetrahydrofurfuryl-(1S)-camphor-10-sulfonate] to N-[(R)-tetrahydrofurfuryl]-etilefrine and subsequent separation of the diastereomers by HPLC. An animal experiment showed that the (R)(-)-enantiomer is more effective.
依托利定(Effortil)的对映体通过对映选择性氢化制备。通过与(+)-[(R)-四氢糠基-(1S)-樟脑-10-磺酸盐]转化为N- [(R)-四氢糠基]-依托利定,然后通过高效液相色谱法分离非对映体来测定光学纯度。一项动物实验表明,(R)(-)-对映体更有效。