Synthesis

Straightforward novel one-pot enaminone and pyrimidine syntheses by coupling-addition-cyclocondensation sequences

AS Karpov, TJJ Müller

Index: Karpov, Alexei S.; Mueller, Thomas J. J. Synthesis, 2003 , # 18 p. 2815 - 2826

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Citation Number: 86

Abstract

Abstract The coupling of acid chlorides 1 with terminal alkynes 2 using only one equivalent (!) of triethylamine under Sonogashira conditions followed by subsequent addition of primary or secondary amines 4 to the intermediate alkynones 3 represents a straightforward one-pot three component access to enaminones 5 under mild conditions and in excellent yields. Furthermore, 2, 4-di-and 2, 4, 6-trisubstituted pyrimidines 7 can be synthesized in ...