4.8 Article

Multicomponent Synthesis of Biologically Relevant S-Aryl Dithiocarbamates Using Diaryliodonium Salts

Journal

ORGANIC LETTERS
Volume 23, Issue 16, Pages 6401-6406

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.1c02220

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Funding

  1. CSIR [02(0426)/21/EMR-II]
  2. SERB [ECR/2017/001410]
  3. DBT [BT/12/IYBA/2019/02]

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The transition-metal-free three-component annulation method provides a convenient and efficient access to biologically relevant S-aryl dithiocarbamates, showing drug-likeness and good ADMET characteristics.
A transition-metal-free one-pot three-component annulation between diaryliodonium triflates, cyclic and acyclic aliphatic amines, and carbon disulfide providing a convenient and efficient access to biologically relevant S-aryl dithiocarbamates is developed. The reaction does not require metal, base, or any other additive and operates under mild and ambient conditions. This methodology is robust, scalable, and exhibits a broad substrate scope. The in silico analysis revealed that the majority of the compounds have a drug-likeness and good ADMET characteristics.

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