2-巯基嘧啶与碳酸Morita-Baylis-Hillman酯的选择性S-烯丙基烷基化

Selective S-Allylic Alkylation of 2-Thiopyrimidine with Morita-Baylis-Hillman Carbonates

发展了一种1,4-二氮杂二环[2.2.2]辛烷(DABCO)催化2-巯基嘧啶与碳酸Morita-Baylis-Hillman(MBH)酯的S-烯丙基烷基化反应新方法.一系列碳酸MBH酯与2-巯基嘧啶反应并以55%~99%的产率得到S-烯丙基烷基化产物.具有专一的化学选择性和良好的区域选择性,反应条件温和,反应时间短,底物适用广泛,有良好的应用前景.

The S-allylic alkylation of 2-thiopyrimidine with Morita-Baylis-Hillman（MBH） carbonates catalyzed by 1,4-diazabicyclo[2.2.2]octane（DABCO） has been developed. A variety of Morita-Baylis-Hillman（MBH） carbonates reacted with 2-thiopyrimidine and gave the desired S-allylic alkylated products in 55%~99% yields with exclusive chemoselectivity and excellent regioselectivity. The mild reaction conditions, short reaction time, and broad substrate scope make this method very practical.