4.8 Article

Transition-Metal-Free Regioselective Cross-Coupling: Controlled Synthesis of Mono- or Dithiolation Indolizines

Journal

ORGANIC LETTERS
Volume 20, Issue 11, Pages 3291-3295

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.8b01168

Keywords

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Funding

  1. National Natural Science Foundation of China [21302023, 21272044]
  2. Innovation and Strong School Project of Guangdong Pharmaceutical University [2015cxqx212]
  3. Science and Technology Planning Project of Guangdong Province [2016A010103039, 201806040009, 201804010349]
  4. Provincial Experimental Teaching Demonstration Center of Chemistry & Chemical Engineering

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An efficient transition-metal-free regioselective C-H/S-H cross-coupling of indolizines with thiols has been developed for the first time to describe a workable route to indolizine thioethers. This finding provides a new method and more straightforward pathway for controllable synthesis of mono- or dithiolation indolizines that are otherwise difficult to obtain by the literature methods. The reaction exhibits good functional group tolerance and high efficiency and affords the products in good to excellent yields.

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