433330-81-5Relevant articles and documents
One-pot synthesis of useful heterocycles in medicinal chemistry using a cascade strategy
Wu, Guiyong,Yin, Weiyu,Shen, Hong C.,Huang, Yong
supporting information; experimental part, p. 580 - 585 (2012/04/23)
To access useful heterocycles in medicinal chemistry such as pyridazinones, dihydropyrimidinones, and dihydropyrimidinthiones, a "green" mild and highly efficient one-pot triple cascade was developed involving a Claisen-decarboxylation, electrophilic reaction, and subsequent heterocyclization. In addition, indazoles and benzofurans could also be constructed via a double cascade. To develop the cascade process, a direct Claisen-decarboxylation reaction was firstly optimized. This reaction can then couple with electrophilic reactions including alkylation, Michael addition or aldol reaction to enable the preparation of various aryl ketones in a one-pot fashion. The Royal Society of Chemistry 2012.
Synthesis and SAR of 1,4,5,6-tetrahydropyridazines as potent cannabinoid CB1 receptor antagonists
Lange, Jos H.M.,den Hartog, Arnold P.,van der Neut, Martina A.W.,van Vliet, Bernard J.,Kruse, Chris G.
scheme or table, p. 5675 - 5678 (2010/04/05)
The synthesis and structure-activity relationship studies of 1,4,5,6-tetrahydropyridazines are described. The target compounds 3-5 represent a novel class of potent and selective CB1 receptor antagonists.
Mono- and di-substituted 5,6-diphenyl-3-alkylaminopyridazines active as ACAT inhibitors
Toma, Lucio,Giovannoni, Maria Paola,Dal Piaz, Vittorio,Kwon, Byoung-Mog,Kim, Young-Kook,Gelain, Arianna,Barlocco, Daniela
, p. 39 - 46 (2007/10/03)
A series of mono- or di-para-substituted 5,6-diphenyl-3-alkylaminopyridazines were synthesized and their inhibitory activity against acyl-CoA:cholesterol acyltransferase (ACAT) was tested on the enzyme prepared from rat liver microsomes. The compound which combines a chlorine atom on the 6-phenyl ring and a n-hexylamino chain showed a significant enhancement of activity with respect to the unsubstituted derivative. Attempts to correlate the activity of the compounds to their structural features, also through theoretical calculations, are reported.