钯催化二肽中苯丙氨酸部分的分子内 C(sp)-H 胺化反应：含吲哚啉-2-羧酸酯的二肽的合成。
Pd-catalyzed intramolecular C(sp)-H amination of phenylalanine moieties in dipeptides: synthesis of indoline-2-carboxylate-containing dipeptides.
机构信息
State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 501 Haike Road, Zhangjiang Hi-Tech Park, Shanghai 201203, China.
出版信息
Org Biomol Chem. 2018 Apr 4;16(14):2402-2405. doi: 10.1039/C8OB00207J.
A palladium-catalyzed intramolecular C(sp2)-H amination of phenylalanine moieties in dipeptides is described. By this protocol, a series of indoline-2-carboxylate-containing dipeptides were synthesized from dipeptides. The N-protected amino acid moiety within the peptide is used as an intrinsic bidentate directing group. This intramolecular C-H amination reaction provides an appealing strategy for the post-synthetic modification of peptides.
本文描述了钯催化的二肽中苯丙氨酸部分的分子内 C(sp2)-H 胺化反应。通过该方案，从二肽合成了一系列含吲哚啉-2-羧酸酯的二肽。肽中的 N-保护氨基酸部分用作内在双齿导向基团。这种分子内 C-H 胺化反应为肽的后期合成修饰提供了一种有吸引力的策略。
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