P(NMe2)3‑Mediated Regioselective
N‑Alkylation of 2‑Pyridones via Direct Deoxygenation
of α‑Keto Esters

Wang, Nan; Huang, Yuanyuan; Zi, You; Wang, Mengke; Huang, Weichun

doi:10.1021/acs.joc.3c02819.s001

jo3c02819_si_001.pdf (3.02 MB)

P(NMe₂)₃‑Mediated Regioselective N‑Alkylation of 2‑Pyridones via Direct Deoxygenation of α‑Keto Esters

journal contribution

posted on 2024-02-17, 14:30 authored by Nan Wang, Yuanyuan Huang, You Zi, Mengke Wang, Weichun Huang

A practical and regioselective direct N-alkylation of 2-pyridones is enabled by use of α-keto esters in the P(NMe₂)₃-mediated deoxygenation process. The reaction proceeds under mild conditions to produce N-alkylated 2-pyridones with high selectivity and generality, and the protocol is shown to be applicable for the scale-up synthesis, which makes it promising for practical applications.