Tetrahedron Letters

Chemically enabled synthesis of 2-amino-4-heteroarylpyrimidines

PS Humphries, QQT Do, DM Wilhite

Index: Humphries, Paul S.; Do, Quyen-Quyen T.; Wilhite, David M. Tetrahedron Letters, 2009 , vol. 50, # 21 p. 2552 - 2554

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Citation Number: 4

Abstract

2-Amino-4-heteroarylpyrimidines were initially synthesized by microwave-induced SNAr reactions of primary alkyl amines and 2-methylsulfonylpyrimidines or 2-chloropyrimidines. Following this methodology, pendant piperidine functionality was elaborated utilizing silica- bound reagents in microwave-assisted reductive amination and amide bond formation protocols. These methods proved to be versatile, efficient, and amenable to parallel ...