Scott William L, Zhou Ziniu, Martynow Jacek G, O'Donnell Martin J
Department of Chemistry and Chemical Biology, Indiana University Purdue University Indianapolis, Indianapolis, Indiana 46202-3274, USA.
Org Lett. 2009 Aug 20;11(16):3558-61. doi: 10.1021/ol901279v.
A new solid-phase synthesis efficiently incorporates three different substituents (from R(1)-X, R(2)-CO(2)H, and R(3)-NH(2)) into a glycine-based peptidomimetic scaffold. The synthetic sequence is general and is typically accomplished in >50% overall isolated yield. Alkylating agents with a range of reactivities and normal and branched primary amines give good results. Utility was demonstrated by the synthesis of a series of protected phosphotyrosine mimetics.
一种新的固相合成方法能够有效地将三种不同的取代基（来自R(1)-X、R(2)-CO₂H和R(3)-NH₂）引入基于甘氨酸的拟肽支架中。该合成序列具有通用性，总体分离产率通常>50%。具有一系列反应活性的烷基化剂以及正构和支链伯胺均能产生良好的结果。通过合成一系列受保护的磷酸酪氨酸模拟物证明了其实用性。
