A general and expedient method for the solid-phase synthesis of structurally diverse 1-phenylpyrazolone derivatives

被引:1
|
作者
Tietze, LF
Steinmetz, A
机构
关键词
solid-phase synthesis; combinatorial chemistry; alkylation; enolates; pyrazolones; beta-ketoester;
D O I
暂无
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
The dianion of polymer-bound acetoacetate 3 was generated and trapped with various alkylating agents 5 to give the corresponding gamma-alkylated beta-ketoesters 8 exclusively. Subsequent reaction with phenylhydrazine resulted in cyclization with concomitant cleavage from the polymeric support to afford the 1-phenyl-pyrazolones 10 in high purity and good yield. The ease and generality of this approach is demonstrated by the synthesis of several diverse 1-phenyl-pyrazolones.
引用
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页码:667 / &
页数:3
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