Rapid parallel synthesis of combinatorial libraries of substituted 3-thio-1,2,4-triazoles and 2-thioimidazoles

被引：16

作者：

Theoclitou, ME ^{[1
]}

Delaet, NGJ ^{[1
]}

Robinson, LA ^{[1
]}

机构：

[1] Bristol Myers Squibb Co, Pharma Res Labs, San Diego, CA 92121 USA

来源：

JOURNAL OF COMBINATORIAL CHEMISTRY | 2002年 / 4卷 / 04期

关键词：

D O I：

10.1021/cc010094o

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

Combinatorial libraries of substituted 3-thio-1,2,4-triazoles and 2-thioimidazoles were synthesized in good yield by alkylation of the products via the reaction of isothiocyanates and carboxylic acid hydrazides or beta-aminoketones, respectively. A total of 275 3-thin-1,2,4-triazoles and 283 2-thioimidazoles were synthesized out of the attempted 288 in each case. Most the yields were between 45% and 98%, and all the compounds synthesized were purified to >85% purity. Variations in yields revealed no definitive trends and were mainly attributed to bulky alkylating agents used and the plate well location of the reaction mixtures.

引用

页码：315 / 319

页数：5