Three-component synthesis of 1,4-diazepin-5-ones and the construction of γ-turn-like peptidomimetic libraries

Three-component synthesis of 1,4-diazepin-5-ones and the construction of γ-turn-like peptidomimetic libraries
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DOI:
10.1021/cc700174c
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发表时间:
2008-03-01
影响因子:
--
通讯作者:
Aube, Jeffrey
Aube, Jeffrey
中科院分区:
其他
文献类型:
--
作者:
Fenster, Erik;Rayabarapu, Dinesh K.;Aube, Jeffrey

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已经通过两种制备1,4-二氮杂卓-5-酮的方法证明了γ-转角启发的肽模拟物文库的平行合成。在第一种方法中,以克规模制备1,4-二氮杂卓-5-酮支架,随后多样化以产生文库。在第二种方法中,1,4-二氮杂卓-5-酮的文库直接通过三组分策略产生,该策略最大化在单个步骤中获得的多样性。
The parallel synthesis of gamma-turn-inspired peptidomimetic libraries has been demonstrated through two approaches toward the preparation of 1,4-diazepin-5-ones. In the first approach, 1,4-diazepin-5-ones scaffolds were prepared on gram scale and subsequently diversified to produce libraries. In a second approach, libraries of 1,4-diazepin-5-ones were produced directly through a three-component strategy that maximizes the diversity obtained in a single step.