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    • 10. 发明授权
    • Process of isolating enantiomer components from enantiomer mixtures by particle-size-controlled crystallization
    • 通过粒度控制结晶从对映体混合物中分离对映体组分的方法
    • US08846911B2
    • 2014-09-30
    • US13975744
    • 2013-08-26
    • David MaillardGuntram KollerEwgenij WakareskoSabine Gottburg-Reininger
    • David MaillardGuntram KollerEwgenij WakareskoSabine Gottburg-Reininger
    • C07D251/10C07B57/00C07C29/78C07D251/08
    • C07D251/08C07B57/00C07B2200/07C07C29/78C07D251/10C07C33/26
    • The present invention discloses a process for isolating enantiomer components from a mixture of enantiomers through particle-size-controlled crystallization, comprising the steps of: (a) forming a solution of a mixture of enantiomers (R) and (S) in a solvent in the absence of any further additives or agents; (b) seeding the solution of step (a) simultaneously or consecutively with seed crystals of enantiomer (R) and with seed crystals of enantiomer (S), wherein the seed crystals of enantiomer (R) differ in size and/or in quantity from the seed crystals of enantiomer (S) to allow separation of the crystals composed of a mixture enriched with enantiomer (R) from the crystals composed of a mixture enriched with enantiomer (S); (c) inducing simultaneous crystallization of enantiomer (R) and enantiomer (S); and (d) isolating crystals composed of a mixture enriched with enantiomer (R) from crystals composed of a mixture enriched with enantiomer (S) through size separation of the crystals, preferably through sieving, melting or sedimentation, in particular through sieving.
    • 本发明公开了一种通过粒度控制结晶从对映体混合物中分离对映异构体成分的方法,包括以下步骤:(a)在溶剂中形成对映体(R)和(S)的混合物的溶液 没有任何其他添加剂或药剂; (b)同时或连续地与对映异构体(R)的晶种和对映异构体(S)的晶种接种步骤(a)的溶液,其中对映异构体(R)的晶种在大小和/或数量上不同 对映异构体(S)的晶种,以允许由富含对映异构体(S)的混合物组成的晶体分离富含对映异构体(R)的混合物的晶体; (c)诱导对映体(R)和对映体(S)的同时结晶; 特别是通过筛选,通过筛分,熔融或沉淀,通过大小分离晶体,分离由富含对映体(S)的混合物组成的晶体,由富含对映体(R)的混合物构成的晶体。