Synthesis 2017; 49(16): 3775-3793
DOI: 10.1055/s-0036-1588425
paper
© Georg Thieme Verlag Stuttgart · New York

Regioselective Synthesis of 3-Aminoimidazo[1,2-a]pyrimidines with Triflic Anhydride

Robert P. Law
GlaxoSmithKline, Medicines Research Centre, Gunnels Wood Road, Stevenage, SG1 2NY, UK   Email: eric.p.talbot@gsk.com
,
Sabri Ukuser
GlaxoSmithKline, Medicines Research Centre, Gunnels Wood Road, Stevenage, SG1 2NY, UK   Email: eric.p.talbot@gsk.com
,
Daniel T. Tape
GlaxoSmithKline, Medicines Research Centre, Gunnels Wood Road, Stevenage, SG1 2NY, UK   Email: eric.p.talbot@gsk.com
,
Eric P. A. Talbot*
GlaxoSmithKline, Medicines Research Centre, Gunnels Wood Road, Stevenage, SG1 2NY, UK   Email: eric.p.talbot@gsk.com
› Author Affiliations
Further Information

Publication History

Received: 23 April 2017

Accepted after revision: 24 April 2017

Publication Date:
07 June 2017 (online)


Abstract

The regioselective synthesis of 3-aminoimidazo[1,2-a]pyrimidines via triflic anhydride mediated amide activation and intramolecular cyclisation is reported. The nature of the added pyridine base allows access to both regioisomers from a simple common precursor. The method tolerates a range of functional groups and provides access to novel heterocyclic scaffolds.

Supporting Information