4.8 Article

Continuous-Flow Visible Light Organophotocatalysis for Direct Arylation of 2H-Indazoles: Fast Access to Drug Molecules

期刊

CHEMSUSCHEM
卷 12, 期 12, 页码 2581-2586

出版社

WILEY-V C H VERLAG GMBH
DOI: 10.1002/cssc.201900736

关键词

C-H activation; drug synthesis; flow chemistry; organocatalysis; photocatalysis

资金

  1. National Research Foundation (NRF) of Korea - Korean government [NRF-2017R1A3B1023598]

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A continuous-flow homogeneous photocatalytic method has been devised for the direct arylation of 2H-indazoles. This visible-light-promoted approach directly accesses a wide range of structurally diverse C3-arylated scaffolds of biological interest in a fast (1 min), single-step reaction by using eosin Y as an organophotocatalyst. Furthermore, a microreactor technology is also employed for the fast synthesis of liver X receptor inhibitor drugs with very good yields under metal-free conditions, whereas the reported methods required multiple steps and much longer reaction times (18-24 h).

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