A Practical Method for Functionalized Peptide or Amide Bond Formation in Aqueous-Ethanol Media with EDC as Activator
A Practical Method for Functionalized Peptide or Amide Bond Formation in Aqueous-Ethanol Media with EDC as Activator
复制标题
DOI：
10.1021/op800240d
复制
发表时间：
2009-03-01
影响因子：
3.4
通讯作者：
Mitchell, David
中科院分区：
文献类型：
--
作者：
Pu, Yangwei John;Vaid, Radhe K.;Mitchell, David
以乙醇为溶剂，采用方便的一锅法，将酸活化剂N-（3-二甲氨基丙基）-N-乙基碳二亚胺盐酸盐（EDC）简单地加入到羧酸、胺、催化剂HOW（1-羟基苯并三唑）和作为碱的NMM（N-甲基吗啉）的混合物中，选择性地形成酰胺或肽。敏感官能团如羟基在反应条件下耐受良好。此外，产物的分离通常通过从反应介质中简单过滤来进行。对这种方法的范围和一般性进行了调查。
Selective formation of amides or peptides with ethanol as solvent using a convenient one-pot procedure in which acid activating agent N-(3-dimethylaminopropyl)-N-ethylcarbodiimide hydrochloride (EDC) is simply added to a mixture of the carboxylic acid, amine, catalytic HOW (1-hydroxy benzotriazole), and NMM (N-methylmorpholine) as base has been developed. Sensitive functionalities such as hydroxyl groups are well tolerated under the reaction conditions. In addition, isolation of products is usually by simple filtration from the reaction media. The scope and generality of this methodology was investigated.