4.8 Article

One-step synthesis of benzo[b]thiophenes by aryne reaction with alkynyl sulfides

期刊

CHEMICAL SCIENCE
卷 11, 期 35, 页码 9691-9696

出版社

ROYAL SOC CHEMISTRY
DOI: 10.1039/d0sc04450d

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资金

  1. JSPS KAKENHI [JP19K05451, JP18H02104, JP18H04386, 19J14128]
  2. Naito Foundation
  3. Japan Agency for Medical Research and Development (AMED) [JP20am0101098, JP20gm0910007]
  4. Cooperative Research Project of Research Center for Biomedical Engineering
  5. Grants-in-Aid for Scientific Research [19J14128] Funding Source: KAKEN

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An aryne reaction with alkynyl sulfides affording benzo[b]thiophenes is disclosed. A wide range of 3-substituted benzothiophenes were synthesized from easily availableo-silylaryl triflates and alkynyl sulfides in a one-step intermolecular manner. The synthesis of diverse multisubstituted benzothiophene derivatives involving a pentacyclic compound was achieved by virtue of the good functional group tolerance and versatile C2 functionalizations.

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