Synthesis of <scp>2‐Trifluoromethyl</scp>‐4‐aminoquinolines via <scp>Heating‐Promoted</scp> Multi‐component Reaction of <scp>CF₃‐Imidoyl</scp> Sulfoxonium Ylides and Amines with Difluorocarbene as a <scp>C1</scp> Synthon†

A thermally-induced multi-component reaction of CF3-substituted imidoyl sulfoxonium ylides (TFISYs), amines and (triphenylphosphonio)difluoroacetate (PDFA) has been developed, allowing a facile access to 2-trifluoromethyl-4-aminoquinolines in high yields. The proceeds smoothly with or without the addition sulfur utilizes difluorocarbene as C1 synthon under simply heating conditions. Mechanistic study reveals that in-situ generated thiocarbonyl fluoride, isothiocyanate gem-difluoroalkene might act key intermediates. This article is protected by copyright. All rights reserved. Supporting Information Please note: publisher not responsible for content functionality any supporting information supplied authors. Any queries (other than missing content) should be directed corresponding author article.