Synlett 2014; 25(07): 935-938
DOI: 10.1055/s-0033-1340860
letter
© Georg Thieme Verlag Stuttgart · New York

Microwave-Assisted Synthesis of 4-Substituted 2-Methylthiopyrimidines

Andreas Thomann
a   Helmholtz-Institute for Pharmaceutical Research Saarland, Saarland University, Campus C2.3, 66123 Saarbrücken, Germany   Fax: +49(681)30270308   eMail: rolf.hartmann@helmholtz-hzi.de
,
Carsten Börger
b   PharmBioTec GmbH, Saarland University, Science Park 1, 66123 Saarbrücken, Germany
,
Martin Empting
a   Helmholtz-Institute for Pharmaceutical Research Saarland, Saarland University, Campus C2.3, 66123 Saarbrücken, Germany   Fax: +49(681)30270308   eMail: rolf.hartmann@helmholtz-hzi.de
,
Rolf W. Hartmann*
a   Helmholtz-Institute for Pharmaceutical Research Saarland, Saarland University, Campus C2.3, 66123 Saarbrücken, Germany   Fax: +49(681)30270308   eMail: rolf.hartmann@helmholtz-hzi.de
c   Pharmaceutical and Medicinal Chemistry, Saarland University, Campus C2.3, 66123 Saarbrücken, Germany
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Publikationsverlauf

Received: 06. Januar 2014

Accepted after revision: 04. Februar 2014

Publikationsdatum:
24. März 2014 (online)


Abstract

Typically, SNAr reactions at 4-chloro-2-methylthiopyrimidine are carried out employing DMF and sodium hydride under inert gas as well as prolonged reaction times. Herein, we describe a mild and rapid microwave-assisted synthesis to achieve 4-substituted 2-methylthiopyrimidnes from the corresponding chlorine precursor. Moderate to excellent yields were obtained in a green chemistry fashion requiring only few minutes of reaction time.

Supporting Information