TiCl4-Mediated Preparation of Thiophthalide Derivatives via Formal Thio-Passerini Reactions

  • Sudipta Ponra
  • , Aude Nyadanu
  • , Laurent El Kaïm
  • , Laurence Grimaud
  • , Maxime R. Vitale

Research output: Contribution to journalArticlepeer-review

Abstract

By the formal extension of the Passerini reaction to thiocarbonyl derivatives, the straightforward preparation of thiophthalides is disclosed. This method involves the intermediate formation of a sulfanyl-phthalide and a titanium tetrachloride mediated isocyanide insertion reaction. When tert-butyl thiol is used, thanks to the deprotection of the tert-butyl group, a thiophthalide resulting from a 1,5-Mumm rearrangement is isolated. Owing to the multifaceted activity of TiCl4, all steps may conveniently be performed in one pot, starting directly from 2-formylbenzoic acids, tert-butyl thiol, and various isocyanides.

Original languageEnglish
Pages (from-to)4060-4063
Number of pages4
JournalOrganic Letters
Volume18
Issue number16
DOIs
Publication statusPublished - 19 Aug 2016
Externally publishedYes

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