Synthesis of diverse 4,5-dihydro-3(2H)-pyridazinones on Wang resin

被引:12
作者
Gouault, N [1 ]
Cupif, JF [1 ]
Picard, S [1 ]
Lecat, A [1 ]
David, M [1 ]
机构
[1] Fac Pharm, UPRES Synth & Extract Mol Visee Therapeut, F-35043 Rennes, France
关键词
D O I
10.1211/0022357011776225
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
An efficient solid-phase synthesis of structurally diverse 4,5-dihydro-3(2H)-pyridazinones is described using readily available substituted 4-oxo-butanoic acids. Polymer-supported gamma -ketoesters prepared from Wang resin reacted with several hydrazines to afford the corresponding hydrazones. A protocol developed in mild conditions without isolating the intermediate hydrazone led to pyridazinones in good yields after a cyclization cleavage approach. This successful strategy represents an attractive method for a rapid synthesis of heterocyclic libraries for biological evaluation.
引用
收藏
页码:981 / 985
页数:5
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