Convenient One-Pot Two-Step Synthesis of Symmetrical and Unsymmetrical Diacyl Ureas, Acyl Urea/Carbamate/Thiocarbamate Derivatives, and Related Compounds
Convenient One-Pot Two-Step Synthesis of Symmetrical and Unsymmetrical Diacyl Ureas, Acyl Urea/Carbamate/Thiocarbamate Derivatives, and Related Compounds
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DOI：
10.1055/s-0036-1588724
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发表时间：
2017-05-01
影响因子：
2.6
通讯作者：
Stec, Jozef
中科院分区：
文献类型：
--
作者：
Hernandez, Anolan Garcia;Grooms, Gregory M.;Stec, Jozef
广泛的化学品如酰胺、酰肼、胺、醇、肼基甲酸酯和磺酸酯与由伯酰胺与草酰氯反应生成的酰基异氰酸酯反应，得到对称和不对称的二酰基脲衍生物、酰基脲/氨基甲酸酯/硫代氨基甲酸酯以及相关化合物。该方法提供了从廉价且可商购的起始试剂方便地一锅法、两步合成带有脲、氨基甲酸酯和其它官能团的化合物的手段。预计本报告中提出的结果将扩大药物化学家的工具箱。
A wide range of chemicals such as amides, hydrazides, amines, alcohols, carbazate, and sulfonate were reacted with acyl isocyanates generated by the reaction of primary amides with oxalyl chloride to give symmetrical and unsymmetrical diacyl urea derivatives, acyl ureas/carbamates/thiocarbamates, and related compounds. This method provides means for convenient one-pot, two-step synthesis of compounds bearing urea, carbamate, and other functional groups from cheap and commercially available starting reagents. It is expected that the results presented in this report will expand the medicinal chemist's toolbox.