重新审视环醇：中等大小环肽的简便合成
Cyclols Revisited: Facile Synthesis of Medium-Sized Cyclic Peptides.
作者信息
Mendoza-Sanchez Rodrigo, Corless Victoria B, Nguyen Q Nhu N, Bergeron-Brlek Milan, Frost John, Adachi Shinya, Tantillo Dean J, Yudin Andrei K
机构信息
Davenport Research Laboratories, Department of Chemistry, University of Toronto, 80 St. George St., Toronto, ON, M5S 3H6, Canada.
Department of Chemistry, University of California Davis, 1 Shields Avenue, Davis, CA, USA.
出版信息
Chemistry. 2017 Sep 27;23(54):13319-13322. doi: 10.1002/chem.201703616. Epub 2017 Aug 31.
Medium-sized rings, particularly the corresponding cyclic peptides, are challenging synthetic targets. In the present study, we report an approach to medium-sized cyclic peptides through targeted formation and collapse of cyclol intermediates. This methodology operates on β-amino imides derived from 2,5-diketopiperazines and offers a straightforward transition from frequently examined scaffolds in drug discovery to a rarely visited class of medium-sized rings.
中等大小的环，特别是相应的环肽，是具有挑战性的合成目标。在本研究中，我们报告了一种通过环醇中间体的靶向形成和塌缩来合成中等大小环肽的方法。该方法作用于由2,5-二酮哌嗪衍生的β-氨基酰亚胺，并提供了从药物发现中经常研究的支架到一类很少涉及的中等大小环的直接转变。
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