posted on 2020-03-16, 10:43authored byNgoc Son Le Pham, Hyunik Shin, Jun Yong Kang, Jeong-Hun Sohn
A reaction
method is described for the one-step synthesis of 2-alkynylpyrimidines
from 3,4-dihydropyrimidin-1H-2-thiones (DHPMs) via
dehydrosulfurative Sonogashira cross-coupling with concomitant oxidative
dehydrogenation using a Pd/Cu catalytic system. Together with the
ready availability of DHPMs possessing various substituents at the
C4–C6 positions, this transformation offers rapid and general
access to diverse 2-alkynylpyrimidine derivatives.