Pharmaceutical Institute, Pharmaceutical Chemistry I, University of Bonn, An der Immenburg 4, 53121 Bonn, Germany.
Org Lett. 2013 Feb 1;15(3):448-51. doi: 10.1021/ol3030583. Epub 2013 Jan 15.
Freidinger lactams, possessing a peptide bond configuration locked to Z, are important key elements of conformationally restricted peptidomimetics. In the present work, the C(α)H(i+1) unit has been replaced by N, leading to novel aza-Freidinger lactams. A synthesis to corresponding building blocks and their E-locked analogs is introduced. The versatile buildings blocks reported here are expected to serve as useful elements in peptide synthesis.
具有 Z 型肽键构型锁定的 Freidinger 内酰胺是构象限制型肽模拟物的重要关键元件。在本工作中，C(α)H(i+1)单元被 N 取代，得到了新型的氮杂-Freidinger 内酰胺。介绍了相应的砌块及其 E 型锁的类似物的合成方法。这里报道的多功能砌块有望成为肽合成中的有用元件。
