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通过β-C(sp3)-H键活化实现脂肪族酰胺的β-氨基化
Yu等报道了通过β-C(sp3)—H键活化实现脂肪族酰胺的β-氨基化。根据他们的研究结果，复合物[Pd(allyl)Cl]2和配体tris[3,5-bis(trifluoromethyl)phenyl]phosphine形成催化体系，N-全氟苯基脂肪酰胺直接与钯催化剂作用，从而实现酰胺的β-C(sp3)—H键活化。在此反应中，反应物为α-位有一个甲基或烷基官能团的脂肪族酰胺，反应过程中其甲基上的C(sp3)—H键发生选择性断裂。另外，吗啉和哌嗪等脂环胺修饰的邻苯甲酰羟胺也可以用作胺化试剂，得到的产物能用在生物活性中间体的合成中。值得注意的是，当使用哌啶酮衍生物作为胺化试剂时，通过脱除哌啶酮结构单元可以将其合成产物6转化为β-氨基酸。
