New methodology for the N-alkylation of 2-amino-3-acylthiophenes

L Aurelio, BL Flynn, PJ Scammells

Index: Aurelio, Luigi; Flynn, Bernard L.; Scammells, Peter J. Organic and Biomolecular Chemistry, 2011 , vol. 9, # 13 p. 4886 - 4902

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Citation Number: 6

Abstract

2-Amino-3-acylthiophenes are known to allosterically modulate the A1adenosine receptor and are also used as intermediates in the synthesis of therapeutic agents and pharmacophores such as thienoazepines and thienopyrimidines. The N-alkylation of 2- aminothiophenes has been notoriously difficult to accomplish under mild conditions and there are very few examples of N-alkylated 2-aminothiophenes in the literature, all of ...