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

被引：6

作者：

Tietze, LF

Steinmetz, A

机构：

来源：

SYNLETT | 1996年 / 07期

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 [有机化学]; 081704 [应用化学];

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

页码：667 / &

页数：3

共 26 条

[1]

DRUG DISCOVERY ON THE ASSEMBLY-LINE [J].