Department of Chemistry, Vali-e-Asr University, Rafsanjan, 77176, Iran.
Mol Divers. 2020 Feb;24(1):131-139. doi: 10.1007/s11030-019-09933-8. Epub 2019 Mar 13.
An efficient and simple protocol for the synthesis of trifluoromethylated quinazolines has been described by I-/KI-promoted oxidative C(sp)-C(sp) bond under the optimal oxidative cyclization reaction conditions. The required 2,2,2-trifluoro-N-benzyl-N'-arylacetimidamides are readily prepared from the corresponding acetimidoyl chlorides and benzylamines under a nucleophilic substitution reaction in the form of in situ. The merits of this protocol are the use of inexpensive molecular iodine, metal-free oxidative coupling and good to excellent yields.
描述了一种通过 I-/KI 促进的氧化 C(sp)-C(sp)键形成来合成三氟甲基喹唑啉的有效且简单的方法，在最佳氧化环化反应条件下进行。所需的 2,2,2-三氟-N-苄基-N'-芳基乙二酰胺可通过相应的乙二酰胺氯和苄胺在亲核取代反应中就地以式制备。该方法的优点是使用了廉价的分子碘、无金属氧化偶联和良好至优异的产率。
