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Dehydrosulfurative C–N Cross-Coupling and Concomitant Oxidative Dehydrogenation for One-Step Synthesis of 2‑Aryl(alkyl)aminopyrimidines from 3,4-Dihydropyrimidin‑1H‑2-thiones

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posted on 2016-09-28, 16:53 authored by Nguyen Huu Trong Phan, Hyeji Kim, Hyunik Shin, Hee-Seung Lee, Jeong-Hun Sohn
A method for the synthesis of 2-aryl­(alkyl)­aminopyrimidines from readily available 3,4-dihydropyrimidin-1H-2-thiones (DHPMs) via dehydrosulfurative C–N cross-coupling and concomitant oxidative dehydrogenation under a Pd/Cu catalytic system is described. This reaction protocol provides unprecedented diversity of fully substituted 2-aryl­(alkyl)­aminopyrimidines in a single step from a wide range of DHPMs and amine coupling partners.

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