非天然的γ-氨基酸结构广泛存在于天然产物与药物分子中, 因此通过直接的不对称胺化反应合成非天然氨基酸衍生物具有重要的研究意义和应用价值. 以偶氮二甲酸酯为氮源, 一价银为催化剂, 联苯类轴手性双膦化合物为配体, 高效地实现了偶氮二甲酸酯与β,γ-不饱和酰胺的不对称反应. 该反应具有良好的底物适用性, 以中等的收率获得了一系列的手性γ-氨基酸衍生物, 产物对映选择性可以达到90%.

Unnatural γ-amino acid structures are widely present in natural products and drug molecules. Therefore, the synthesis of unnatural amino acids through direct asymmetric amination reaction has important research and application values. An efficient γ-amination reaction using azodicarboxylate as nitrogen source is reported. The asymmetric reaction of azodicarboxylate with β,γ-unsaturated amides was realized by using monovalent silver as Lewis acid catalyst and biphenyl axial chiral bisphosphine compound as ligand. The reaction has good substrate applicability, and a series of chiral γ-amino acid derivatives were obtained in moderate yields with an enantioselectivity of 90% ee.