Gan Jiangang, Ma Dawei
State Key Laboratory of Bioorganic and Natural Products Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, 354 Fenglin Lu, Shanghai 200032, China.
Org Lett. 2009 Jul 2;11(13):2788-90. doi: 10.1021/ol900943b.
CuI-catalyzed coupling of 4-methylphenyl bromide with amino acids gives N-aryl amino acids, which are converted into linear dipeptides via iodination and condensation with L-cysteine derived acyl chloride. Cyclization is achieved via a CuI/N,N-dimethylglycine catalyzed intramolecular coupling of aryl iodides with the liberated thiol to afford 1,5-benzothiazepine dipeptide mimetics.
碘化亚铜催化4-甲基苯基溴与氨基酸反应生成N-芳基氨基酸，这些氨基酸通过碘化反应以及与L-半胱氨酸衍生的酰氯缩合反应转化为线性二肽。通过碘化亚铜/N,N-二甲基甘氨酸催化芳基碘化物与释放出的硫醇进行分子内偶联反应实现环化，得到1,5-苯并硫氮杂䓬二肽模拟物。
