36244-13-0Relevant articles and documents
FeCl3-Mediated Synthesis of 2-(Trifluoromethyl)quinazolin-4(3 H)-ones from Isatins and Trifluoroacetimidoyl Chlorides
Wang, Le-Cheng,Du, Shiying,Chen, Zhengkai,Wu, Xiao-Feng
, p. 5567 - 5571 (2020)
An FeCl3-mediated cascade coupling/decarbonylative annulation reaction for the efficient construction of 2-(trifluoromethyl)quinazolin-4(3H)-ones has been developed. This transformation employs readily available isatins and trifluoroacetimidoyl chlorides as the starting materials, providing a facile and practical route to diverse biologically relevant quinazolin-4(3H)-one derivatives. A plausible reaction pathway has been proposed based on the mechanistic observations.
Palladium-Catalyzed Carbonylative Synthesis of 2-(Trifluoromethyl)quinazolin-4(3H)-ones from Trifluoroacetimidoyl Chlorides and Nitro Compounds
Wang, Le-Cheng,Zhang, Yu,Chen, Zhengkai,Wu, Xiao-Feng
supporting information, p. 1417 - 1426 (2021/02/01)
A procedure on palladium-catalyzed carbonylative reaction of trifluoroacetimidoyl chlorides and nitro compounds for the construction of pharmaceutically valuable 2-(trifluoromethyl)quinazolin-4(3H)-ones has been achieved. In this transformation, Mo(CO)6 has been used both as a convenient CO source and a reducing reagent. This newly developed protocol is compatible with various nitro compounds and can be readily scaled up to 1 mmol scale. (Figure presented.).
Preparation method of 2-trifluoromethyl substituted quinazolinone compound and application of 2-trifluoromethyl substituted quinazolinone compound in synthesis of pharmaceutical molecules
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Paragraph 0033; 0034; 0035; 0036; 0037; 0038; 0039; 0040, (2021/07/01)
The invention discloses a preparation method of a 2-trifluoromethyl substituted quinazolinone compound. The preparation method comprises the following steps: adding a palladium catalyst, a ligand, a carbon monoxide substitute, an additive, trifluoroethylimido acyl chloride and amine into an organic solvent, reacting at 110 DEG C for 16-30 hours, and after the reaction is completed, carrying out post-treatment to obtain the 2-trifluoromethyl substituted quinazolinone compound. The preparation method has the advantages of simple operation, cheap and easily available initial raw materials, high reaction efficiency, good substrate compatibility, synthesis of trifluoromethyl quinazolinone compounds substituted by different groups through substrate design, convenient operation, and broadening of the practicality of the method. The method is also successfully applied to the high-yield synthesis of the drug molecule Rutaecarpine.