期刊
REACTION CHEMISTRY & ENGINEERING
卷 7, 期 8, 页码 1779-1785出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/d2re00145d
关键词
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资金
- National Natural Science Foundation of China [22071056]
This study has established a highly diastereoselective continuous flow protocol under mild conditions to obtain various functionalized pyrrolidines with rapid, cost-efficient, and scalable access.
An alpha-chiral pyrrolidine library has been established via a highly diastereoselective continuous flow protocol under mild conditions. Various functionalized pyrrolidines have been obtained in generally high yields (up to 87%) and with superior diastereocontrol within 150 s. The utility of this flow methodology is further demonstrated by the gram-scale preparation of a kappa-opioid receptor selective antagonist Aticaprant intermediate. Moreover, the scale-up in a self-designed microfluidic reactor provides a throughput of 7.45 g h(-1), suggesting its potential large-scale applications. The flow procedure affords rapid, cost-efficient, and scalable access to obtain chiral alpha-substituted pyrrolidines in the compound library.
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