Diversification of pharmaceutical molecules via late-stage C(sp2)–H functionalization

C–H late-stage functionalization has gradually become a powerful approach for the rapid optimization of lead compounds’ bioactivity. Significant advances in this field have been achieved in the past few years, mainly, the C–H functionalization system in (hetero)aryl C–H activation owing to the impor...

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Main Authors: Weidong Shang, Hongbao Sun, Wei Chen, Jie Liu
Format: Article
Language:English
Published: KeAi Communications Co. Ltd. 2023-05-01
Series:Green Synthesis and Catalysis
Subjects:
Online Access:http://www.sciencedirect.com/science/article/pii/S2666554922001363
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author Weidong Shang
Hongbao Sun
Wei Chen
Jie Liu
author_facet Weidong Shang
Hongbao Sun
Wei Chen
Jie Liu
author_sort Weidong Shang
collection DOAJ
description C–H late-stage functionalization has gradually become a powerful approach for the rapid optimization of lead compounds’ bioactivity. Significant advances in this field have been achieved in the past few years, mainly, the C–H functionalization system in (hetero)aryl C–H activation owing to the importance of (hetero)aryl moiety in pharmaceutical. In this review, we described the selected recent examples of how developed intermolecular C(sp2)–H functionalization methodologies involving diverse techniques diversify pharmaceutical molecules in the late stage.
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spelling doaj.art-d4f4e774efc14d11982e8d64f28d591d2023-06-07T04:49:56ZengKeAi Communications Co. Ltd.Green Synthesis and Catalysis2666-55492023-05-0142104123Diversification of pharmaceutical molecules via late-stage C(sp2)–H functionalizationWeidong Shang0Hongbao Sun1Wei Chen2Jie Liu3Targeted Tracer Research and Development Laboratory, Institute of Respiratory Health, Huaxi MR Research Center, Laboratory of Clinical Nuclear Medicine, Department of Nuclear Medicine, State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, Chengdu, 610041, ChinaTargeted Tracer Research and Development Laboratory, Institute of Respiratory Health, Huaxi MR Research Center, Laboratory of Clinical Nuclear Medicine, Department of Nuclear Medicine, State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, Chengdu, 610041, ChinaCorresponding author.; Targeted Tracer Research and Development Laboratory, Institute of Respiratory Health, Huaxi MR Research Center, Laboratory of Clinical Nuclear Medicine, Department of Nuclear Medicine, State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, Chengdu, 610041, ChinaCorresponding author.; Targeted Tracer Research and Development Laboratory, Institute of Respiratory Health, Huaxi MR Research Center, Laboratory of Clinical Nuclear Medicine, Department of Nuclear Medicine, State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, Chengdu, 610041, ChinaC–H late-stage functionalization has gradually become a powerful approach for the rapid optimization of lead compounds’ bioactivity. Significant advances in this field have been achieved in the past few years, mainly, the C–H functionalization system in (hetero)aryl C–H activation owing to the importance of (hetero)aryl moiety in pharmaceutical. In this review, we described the selected recent examples of how developed intermolecular C(sp2)–H functionalization methodologies involving diverse techniques diversify pharmaceutical molecules in the late stage.http://www.sciencedirect.com/science/article/pii/S2666554922001363C–H FunctionalizationSynthetic toolLate-stage functionalizationPharmaceutical molecules
spellingShingle Weidong Shang
Hongbao Sun
Wei Chen
Jie Liu
Diversification of pharmaceutical molecules via late-stage C(sp2)–H functionalization
Green Synthesis and Catalysis
C–H Functionalization
Synthetic tool
Late-stage functionalization
Pharmaceutical molecules
title Diversification of pharmaceutical molecules via late-stage C(sp2)–H functionalization
title_full Diversification of pharmaceutical molecules via late-stage C(sp2)–H functionalization
title_fullStr Diversification of pharmaceutical molecules via late-stage C(sp2)–H functionalization
title_full_unstemmed Diversification of pharmaceutical molecules via late-stage C(sp2)–H functionalization
title_short Diversification of pharmaceutical molecules via late-stage C(sp2)–H functionalization
title_sort diversification of pharmaceutical molecules via late stage c sp2 h functionalization
topic C–H Functionalization
Synthetic tool
Late-stage functionalization
Pharmaceutical molecules
url http://www.sciencedirect.com/science/article/pii/S2666554922001363
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