Hou Jinyu, Fan Hongying, Zhang Xue, Liu Xingyu, Chen Jian, Lv Guanghui, He Shiyun, Hai Li, Yang Zhongzhen, Wu Yong
Key Laboratory of Drug-Targeting and Drug Delivery System of the Education Ministry and Department of Medicinal Chemistry, Sichuan Engineering Laboratory for Plant-Sourced Drug and Sichuan Research Center for Drug Precision Industrial Technology, West China School of Pharmacy, Sichuan University, No. 17 Southern Renmin Road, Chengdu, Sichuan 610041, People's Republic of China.
Department of Pharmacy, Hubei Provincial Clinical Research Center for Umbilical Cord Blood Hematopoietic Stem Cells, Taihe Hospital, Hubei University of Medicine, Shiyan 442000, Hubei, China.
Org Lett. 2024 Sep 13;26(36):7638-7643. doi: 10.1021/acs.orglett.4c02742. Epub 2024 Sep 4.
Herein, we disclose a visible-light-driven photoredox-catalyzed protocol for site-selective alkylation of glycine derivatives via 1,2-hydrogen atom transfer, which is distinguished by metal free and mild conditions, high chemoselectivity, and good functional group compatibility. This protocol provides a unique approach for synthesizing valuable α,β-diamino acid derivatives. Furthermore, the potential synthetic merit of this transformation is proven by a scale-up reaction and late-stage functionalization of peptides.
在此，我们披露了一种可见光驱动的光氧化还原催化协议，用于通过1,2-氢原子转移对甘氨酸衍生物进行位点选择性烷基化，该协议具有无金属、条件温和、化学选择性高和官能团兼容性好的特点。该协议为合成有价值的α,β-二氨基酸衍生物提供了一种独特的方法。此外，这种转化的潜在合成优点通过放大反应和肽的后期官能化得到了证明。
