4.7 Article

Ruthenium-catalyzed enantioselective hydrogenation of quinoxalinones and quinazolinones

期刊

ORGANIC CHEMISTRY FRONTIERS
卷 9, 期 2, 页码 400-406

出版社

ROYAL SOC CHEMISTRY
DOI: 10.1039/d1qo01598b

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资金

  1. National Natural Science Foundation of China [21871270, 21790332, 21521002]
  2. CAS [QYZDJSSWSLH023]
  3. Youth Innovation Promotion Association, Chinese Academy of Sciences [201708]

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An efficient Ru-catalyzed enantioselective hydrogenation method has been successfully developed for the synthesis of chiral dihydroquinoxalinones and dihydroquinazolinones with excellent results (89-98% yields, up to 98% ee). Additionally, a key enantiopure dihydroquinoxalinone intermediate towards the synthesis of a bioactive BRD4 inhibitor was conveniently synthesized using this catalytic hydrogenation methodology.
An efficient Ru-catalyzed enantioselective hydrogenation of quinoxalinone and quinazolinone derivatives has been successfully developed, providing a straightforward and facile access to chiral dihydroquinoxalinones and dihydroquinazolinones with excellent results (89-98% yields, up to 98% ee). Importantly, the key enantiopure dihydroquinoxalinone intermediate towards the synthesis of a bioactive BRD4 inhibitor was conveniently synthesized by this catalytic hydrogenation methodology.

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