Solid-phase syntheses of 1,2,4-trisubstituted urazole and thiourazole derivatives

被引：10

作者：

Phoon, CW ^{[1
]}

Sim, MM ^{[1
]}

机构：

[1] Inst Mol & Cell Biol, Med & Combinatorial Chem Lab, Singapore 117609, Singapore

来源：

JOURNAL OF COMBINATORIAL CHEMISTRY | 2002年 / 4卷 / 05期

关键词：

D O I：

10.1021/cc0200134

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

Solid-phase syntheses of 1,2,4-trisubstituted urazole and thiourazole derivatives have been accomplished. The synthesis began with the coupling of carbonylimidazole-Wang resin with a disubstituted hydrazine. The resultant carbazate was coupled with an isocyanate or isothiocyanate. Subsequent heating of the resin in the presence of triethylamine or potassium t-butoxide induced cyclization and released the desired (thio)urazole into solution. Most of the products were obtained in high yields and purities. Structural diversity can be further expanded at the R-2 substituent by performing the palladium-mediated Suzuki coupling reaction.

引用

页码：491 / 495

页数：5

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