Kellogg Richard M, Kaptein Bernard, Vries Ton R
Syncom BV, Kadijk 3, 9747, Groningen AT, The Netherlands,
Top Curr Chem. 2007;269:159-97. doi: 10.1007/128_2006_095.
An overview is given of the principles of Pasteur resolutions via separation of diastereomeric salts.Thereafter, primary nucleation processes of (chiral) organic compounds in supersaturated solution are consideredfollowed by crystal growth in the presence of tailor-made additives. A representative example of a DutchResolution is presented, the concept of families of resolving agents is defined and examples are given.The phenomenon of reversed Dutch Resolution, resolution of mixtures of families of racemates, is illustrated.The roles of both solid solution formation and nucleation inhibition in Dutch Resolution are discussed.The work is concluded with the results of a broadly based search for nucleation inhibitors for phenylethylamine as resolving agent. This search can serve as a model for the discovery of nucleation inhibitorsfor other resolving agents. The specific role of bifunctional family members of resolving agents as possiblenucleation inhibitors is also discussed.
本文概述了通过非对映体盐分离进行巴斯德拆分的原理。此后，考虑了（手性）有机化合物在过饱和溶液中的初级成核过程，接着是在定制添加剂存在下的晶体生长。给出了一个荷兰拆分的代表性例子，定义了拆分剂家族的概念并给出了示例。阐述了反向荷兰拆分现象，即外消旋体家族混合物的拆分。讨论了固溶体形成和成核抑制在荷兰拆分中的作用。文章最后给出了以苯乙胺为拆分剂广泛寻找成核抑制剂的结果。该寻找过程可作为发现其他拆分剂成核抑制剂的模型。还讨论了拆分剂双功能家族成员作为可能的成核抑制剂的具体作用。
