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用于受阻羧酸和低亲核性胺反应的缩合试剂
氯-N,N,N',N'-四甲基甲脒六氟磷酸盐 (TCFH, 1) 作为一种缩合试剂被用于空间受阻的羧酸和胺的反应中。室温条件下,在将1-甲基咪唑用作活化剂的羧酸和胺的反应中加入1,即可发生反应并高产率的得到相应的胺。该反应不仅适用于缬氨酸,S-保护的半胱氨酸等空间受阻的氨基酸,也适用于亲核性低的苯胺衍生物,并且几乎不会发生差向异构化。这些优良的合成特性,使得1可以应用于肽的放大合成,肽类候选药物的开发,以及肽的自动化合成中。
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- TCFH−NMI: Direct Access to N-Acyl Imidazoliums for Challenging Amide Bond Formations