Synlett 2008(3): 359-362  
DOI: 10.1055/s-2008-1032067
LETTER
© Georg Thieme Verlag Stuttgart · New York

Rapid One-Pot Synthesis of Antiparasitic Quinolines Based upon the Microwave-Assisted Coupling-Isomerization Reaction (MACIR)

Oana G. Schramma, Thomas Oesera, Marcel Kaiserb, Reto Brunb, Thomas J. J. Müller*a,1
a Organisch-Chemisches Institut, Ruprecht-Karls-Universität Heidelberg, Im Neuenheimer Feld 270, 69120 Heidelberg, Germany
b Schweizerisches Tropeninstitut, Socinstraße 57, Postfach, 4002 Basel, Switzerland
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Publikationsverlauf

Received 5 November 2007
Publikationsdatum:
23. Januar 2008 (online)

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Abstract

2-Substituted quinolines and related derivatives can be rapidly prepared from (hetero)aryl halides and propargyl alcohols in the sense of a one-pot microwave-assisted coupling-isomerization reaction (MACIR). First biological tests against trypanosomes and protozoans have revealed antiparasitic activity in the lower micromolar range.