Département de Chimie, Université de Montréal , C.P. 6128, Succursale Centre-Ville, Montréal, Québec H3C 3J7, Canada.
Org Lett. 2014 Jan 3;16(1):298-301. doi: 10.1021/ol403297v. Epub 2013 Dec 13.
Copper catalyzed coupling of Mannich reagents to aza-propargylglycine residues has been employed to synthesize constrained aza-lysine peptides. Employing growth hormone releasing peptide-6 (GHRP-6) as a model peptide and a variety of secondary amines, 18 aza-Lys analogs were synthesized by this so-called A(3)-coupling reaction. This effective method for making constrained aza-Lys-peptides offers strong potential for exploring various recognition events implicating lysine residues including post-translational peptide modification.
铜催化的曼尼希试剂与氮丙啶基甘氨酸残基的偶联反应已被用于合成约束性氮赖氨酸肽。使用生长激素释放肽-6（GHRP-6）作为模型肽和各种仲胺，通过所谓的 A（3）-偶联反应合成了 18 种氮赖氨酸类似物。这种合成约束性氮赖氨酸肽的有效方法为探索涉及赖氨酸残基的各种识别事件提供了强大的潜力，包括翻译后肽修饰。
