Efficient assembly of 2,5,6-substituted pyrimidines via MgI(2)-mediated Morita-Baylis-Hillman reaction.

Efficient assembly of 2,5,6-substituted pyrimidines via MgI(2)-mediated Morita-Baylis-Hillman reaction.
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通过 MgI(2) 介导的 Morita-Baylis-Hillman 反应有效组装 2,5,6-取代的嘧啶。

DOI:
10.1021/cc100001e
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发表时间:
2010
影响因子:
--
通讯作者:
McLaughlin,MarkL
McLaughlin,MarkL
中科院分区:
--
文献类型:
--
作者:
Sharma,Vasudha;McLaughlin,MarkL

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A mild and efficient protocol for the synthesis of a 2,6-disubstituted pyrimidine-5-carboxylate library via a Morita−Baylis−Hillman (MBH) adduct is described. Herein, the three step methodology involves the use of substituted α-iodomethylene β-keto ester intermediates obtained after oxidation of the MBH adducts, which are condensed with various types of amidine or guanidine derivatives, to generate the 2, 6-disubstituted pyrimidines-5-carboxylate libraries.