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Construction of an α-chiral pyrrolidine library with a rapid and scalable continuous flow protocol
Reaction Chemistry & Engineering ( IF 3.4 ) Pub Date : 2022-05-16 , DOI: 10.1039/d2re00145d Chao Shan 1 , Liming Cao 1 , Jiasheng Yang 1 , Ruihua Cheng 2 , Xiantong Yao 2 , Chaoming Liang 2 , Maolin Sun 2 , Jinxing Ye 1, 2
Reaction Chemistry & Engineering ( IF 3.4 ) Pub Date : 2022-05-16 , DOI: 10.1039/d2re00145d Chao Shan 1 , Liming Cao 1 , Jiasheng Yang 1 , Ruihua Cheng 2 , Xiantong Yao 2 , Chaoming Liang 2 , Maolin Sun 2 , Jinxing Ye 1, 2
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An α-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 κ-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 α-substituted pyrrolidines in the compound library.
中文翻译：
具有快速且可扩展的连续流动协议的α-手性吡咯烷库的构建
在温和条件下，通过高度非对映选择性连续流动协议建立了 α-手性吡咯烷库。各种官能化的吡咯烷通常以高产率（高达 87%）获得，并且在 150 秒内具有优异的非对映控制。κ-阿片受体选择性拮抗剂 Aticaprant 中间体的克级制备进一步证明了这种流动方法的实用性。此外，自行设计的微流控反应器中的放大提供了 7.45 gh -1的吞吐量，表明其潜在的大规模应用。流动程序提供了快速、经济高效和可扩展的访问，以在化合物库中获得手性 α-取代吡咯烷。
更新日期：2022-05-16
中文翻译：
具有快速且可扩展的连续流动协议的α-手性吡咯烷库的构建
在温和条件下，通过高度非对映选择性连续流动协议建立了 α-手性吡咯烷库。各种官能化的吡咯烷通常以高产率（高达 87%）获得，并且在 150 秒内具有优异的非对映控制。κ-阿片受体选择性拮抗剂 Aticaprant 中间体的克级制备进一步证明了这种流动方法的实用性。此外，自行设计的微流控反应器中的放大提供了 7.45 gh -1的吞吐量，表明其潜在的大规模应用。流动程序提供了快速、经济高效和可扩展的访问，以在化合物库中获得手性 α-取代吡咯烷。
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