An easy two step synthesis of macrocyclic peptidotriazoles via a four-component reaction and copper catalyzed intramolecular azide-alkyne [3+2] click cycloaddition
- 作者：D. Bahulayan ; bahulayan@yahoo.com ; S. Arun
- 关键词：Macrocycles ; Peptidotriazoles ; Click chemistry ; Multi-component reactions ; Step economy
- 刊名：Tetrahedron Letters
- 出版年：2012
- 期刊代码：109_00404039
- 类别：ch
- 出版时间：6 June, 2012
- 卷：53
- 期：23
- 页码：2850-2855
- 文件大小：3024 K
摘要
A two-step macrocyclization strategy for the synthesis of 12- and 14-membered cyclic peptidotriazoles by combining a one pot four-component reaction and an intramolecular [3+2] azide-alkyne click cycloaddition reaction is described. Macrocycles are obtained in good to excellent yield from the aqueous work-up of the reaction mixture and it is possible to expand or contract the ring size by adjusting the length of the nitrile moiety used in the MCR stage.