<i>cis</i>-Apa: A Practical Linker for the Microwave-Assisted Preparation of Cyclic Pseudopeptides via RCM Cyclative Cleavage
作者:Alice Baron、Pascal Verdié、Jean Martinez、Frédéric Lamaty
DOI:10.1021/jo101629v
日期:2011.2.4
linker cis-5-aminopent-3-enoic acid (cis-Apa) was prepared for the synthesis of cyclic pseudopeptides by cyclization−cleavage by using ring-closing methatesis (RCM). We developed a new synthetic pathway for the preparation of the cis-Apa linker that was tested in the cyclization−cleavage process of different RGD peptide sequences. Different macrocyclic peptidomimetics were prepared by using this integrated
制备了一种新的顺式-5-氨基戊-3-烯酸连接体(顺式-Apa),用于通过环合甲基化作用(RCM)通过环化裂解合成环状假肽。我们为制备顺式-Apa接头开发了一条新的合成途径,该途径已在不同RGD肽序列的环化裂解过程中进行了测试。通过使用这种集成的微波辅助方法,制备了不同的大环拟肽,表明易于获得的顺式-Apa氨基酸非常适合作为环化裂解过程中的连接基。