Selective Pyridine-Directed C-H Activation Enabled Synthesis of Pyridine-pyridone α-Helix Mimics

被引：0

作者：

Xiao, Dong ^{[1
]}

Song, Zhiguo J. ^{[2
]}

Song, Zhiyan ^{[3
]}

机构：

[1] Merck & Co Inc, Discovery Chem, 33 Ave Louis Pasteur, Boston, MA 02115 USA

[2] Merck & Co Inc, Proc Res & Dev, 2025 E Scott Ave, Rahway, NJ 07065 USA

[3] Pharmarom Beijing Co Ltd, Dept Synthet Chem, Beijing 100176, Peoples R China

来源：

SYNLETT | 2025年

关键词：

Rh-catalyzed C-H activation; reaction mechanisms; selectivity; C-H activation; heterocycle synthesis; alpha-helix mimics; PALLADIUM-CATALYZED ALKYLATION; PROTEIN-PROTEIN; MODULAR SYNTHESIS; BONDS; FUNCTIONALIZATION; INHIBITORS; MIMETICS; PEPTIDES; LIGANDS; DESIGN;

D O I：

10.1055/s-0043-1775435

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

The exploration of pyridine-directed C-H activation in 2benzyl-6-phenylpyridine revealed selective bromination at the ortho- phenyl position via Rh catalysis, rather than the ortho-benzyl position. In contrast, the corresponding alkylation was unsuccessful, suggesting a preference for the Rh(III) pathway to minimize steric congestion from pyridine disubstitution. This mechanistic insight facilitated the development of a room-temperature C-H activation-bromination method, enabling the synthesis of a pyridine-pyridone alpha-helix mimic.

引用

页数：5

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