Hernández D, Boto A, Guzmán D, Alvarez E
Instituto de Productos Naturales y Agrobiología del CSIC, Avda. Astrofísico Francisco Sánchez 3, 38206-La Laguna, Tenerife, Spain.
Org Biomol Chem. 2017 Sep 26;15(37):7736-7742. doi: 10.1039/c7ob02033c.
An efficient, metal-free synthesis of unusual α-keto γ-amino esters from α-amino acids is achieved by a radical scission-oxidation-addition of silyloxy acrylates procedure, where no purification of the reaction intermediates is needed. This protocol can be applied to the selective modification of the C-terminal position in peptides to give α,γ-hybrids.
通过硅氧基丙烯酸酯的自由基断裂-氧化加成过程,实现了一种高效、无金属的由α-氨基酸合成不寻常的α-酮基γ-氨基酯的方法,该过程无需对反应中间体进行纯化。此方案可应用于肽的C端位置的选择性修饰,以得到α,γ-杂合物。