化学
外消旋化
吡咯烷
产量(工程)
分辨率(逻辑)
酒石酸
过程(计算)
有机化学
组合化学
计算机科学
操作系统
人工智能
冶金
材料科学
柠檬酸
作者
Chuan‐Qi Duan,Siju Bi,Ting Tian,Ting Zhou,Kuaile Lin,Weicheng Zhou
摘要
Abstract ( S )‐2‐(3,5‐dimethylphenyl)pyrrolidine(( S )‐ 1 ), a key intermediate in the synthesis of aticaprant, was effectively prepared via a recycle process of resolution/racemization. The desired ( S )‐ 1 was obtained by resolution of its racemate with D ‐tartaric acid and some alkaline conditions were screened to racemize the undesired ( R )‐ 1 in the resolution mother liquor, and the best (in DMSO with KOH) was identified. Finally, the desired freebase ( S )‐ 1 was obtained in a yield of 63.6% with excellent enantioselectivity (98.7% ee) after three times of recycle process.
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