Transition??Metal??Free Approach to 4??Ethynylpyrimidines via Alkenynones

…, AS Pankova, MA Kuznetsov

Index: Golubev, Pavel R.; Pankova, Alena S.; Kuznetsov, Mikhail A. European Journal of Organic Chemistry, 2014 , vol. 2014, # 17 p. 3614 - 3621

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Citation Number: 2

Abstract

Abstract A practical approach to the synthesis of 4-ethynylpyrimidines by the condensation of arylamidines with 2-aryl-1-ethoxy-5-(trimethylsilyl) pent-1-en-4-yn-3-ones has been developed. As these latter ketones are easily accessible from bis (trimethylsilyl) acetylene and arylacetyl chlorides, the regioselective condensation reported herein provides a facile access to both TMS-protected and unprotected 4-ethynylpyrimidines in yields of up to 85%.