以2-甲硫基苯胺为原料,通过酰化、碘环化以及Suzuki交叉偶联反应,合成了5-甲基-2,3-二苯基-1,5-苯并硫氮杂卓-4(5H)-酮.分别考察了催化剂对酰化反应、溶剂对碘环化反应的影响,以及催化剂、配体、碱和温度等因素对Suzuki交叉偶联反应的影响,在最佳的反应条件下,反应总收率为68.5%,中间产物和目标产物的结构经IR、NMR和MS等测试技术得以确证.
5-Methyl-2,3-diphenyl-1,5-benzothiazepin-4(5H)-one was synthesized via the acylation reaction and iodocyclization reaction and Suzuki cross-coupling reaction with 2-(methylthio)aniline as the initial material. Effects including catalysts on acylation reaction, solvents on iodocyclization and catalysts, ligand, base and reaction temperature on Suzuki cross-coupling reaction have been investigated. Under optimum conditions, the yield of the product was up to 68.5%. The chemical structures of the intermediates and target product were characterized by IR, NMR and MS spectra.
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