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研究了用手性助剂冰片与 5 羟基 2 (5H) 呋喃酮 (1)缩醛化制得液体差向异构体混合物 5[(1S) 内型冰片氧基 ] 2 (5H) 呋喃酮 (4 (R) +4(S) ) (n(4 (R) )∶n(4 (S) ) =50∶50 ) ,以该混合物为底物与硫酚 (醇 )进行不对称Michael加成 ,得到 7对非对映异构体混合物 ,其中 1对固体产物 (6d(R) +6d(S) )经分步结晶分离得 6d(S) ,d .e .大于 98% .此研究为由液体差向异构体混合物获得光学纯非对映异构体提供了一种新方法 .
In this paper, the liquid isomer mixture of 5 [(1S) endoiloxy] 2 (5H) phthalazinone was synthesized by the acetalization of the chiral auxiliary borneol with 5-hydroxy 2 (5H) 4 (S)) (n (4 (R)): n (4 (S)) = 50:50) was subjected to an asymmetric Michael addition reaction with thiophenol To give a mixture of 7 pairs of diastereomers, wherein 6 pairs of solid products (6d (R) + 6d (S)) were separated by fractional crystallization for 6 days A new approach is provided for obtaining optically pure diastereomers from liquid epimeric mixtures.