Synthesis 2014; 46(07): 947-954
DOI: 10.1055/s-0033-1340664
paper
© Georg Thieme Verlag Stuttgart · New York

Mild and Direct Access to 7-Substituted-4-trifluoromethylpyrimido[1,2-b]pyridazin-2-one Systems

Julien Petrignet
Laboratoire d’Infectiologie et Santé Publique (UMR Université François Rabelais/INRA 1282), Université François Rabelais, Faculté des Sciences, Parc de Grandmont, 37200 Tours, France   Fax: +33(2)47367073   Email: mohamed.abarbri@univ-tours.fr
,
Emilie Thiery
Laboratoire d’Infectiologie et Santé Publique (UMR Université François Rabelais/INRA 1282), Université François Rabelais, Faculté des Sciences, Parc de Grandmont, 37200 Tours, France   Fax: +33(2)47367073   Email: mohamed.abarbri@univ-tours.fr
,
Laurence Silpa
Laboratoire d’Infectiologie et Santé Publique (UMR Université François Rabelais/INRA 1282), Université François Rabelais, Faculté des Sciences, Parc de Grandmont, 37200 Tours, France   Fax: +33(2)47367073   Email: mohamed.abarbri@univ-tours.fr
,
Mohamed Abarbri*
Laboratoire d’Infectiologie et Santé Publique (UMR Université François Rabelais/INRA 1282), Université François Rabelais, Faculté des Sciences, Parc de Grandmont, 37200 Tours, France   Fax: +33(2)47367073   Email: mohamed.abarbri@univ-tours.fr
› Author Affiliations
Further Information

Publication History

Received: 18 November 2013

Accepted after revision: 20 December 2013

Publication Date:
30 January 2014 (eFirst)

Abstract

New and efficient methods for the synthesis of 7-substituted-4-trifluoromethylpyrimido[1,2-b]pyridazin-2-one derivatives using either two-step Suzuki/heterocyclization, or two-step heterocyclization/substitution sequences are developed. A variety of substituted products are obtained in good to excellent yields from 3-amino-6-chloropyridazine and ethyl 4,4,4-trifluorobut-2-ynoate.

Supporting Information

 
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