Application of divergent multi-component reactions in the synthesis of a library of peptidomimetics based on γ-amino-α,β-cyclopropyl acids
Application of divergent multi-component reactions in the synthesis of a library of peptidomimetics based on γ-amino-α,β-cyclopropyl acids
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DOI：
10.1016/j.tet.2005.09.016
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发表时间：
2005-11-28
期刊：
影响因子：
2.1
通讯作者：
Twining, LA
中科院分区：
文献类型：
--
作者：
Wipf, P;Werner, S;Twining, LA
将有机二茂锆、醛胺和类碳锌的多组分缩合反应应用于环丙烷氨基酸衍生物的立体选择性合成。这些化合物为46个成员的文库的制备提供了支架。环丙烷氨基酸衍生物的c端和n端分别通过与10种胺和10种酰化剂的缩合而多样化。为了提高产率和加速文库的合成，大多数产物是在微波照射下制备的，并通过聚合物结合清除剂和SPE方法纯化。采用LC-MS对所有化合物进行分析，并对有代表性的化合物进行了表征。(c) 2005 Elsevier Ltd版权所有。
The multi-component condensation of organozirconocene, aldimine and zinc carbenoid was applied to the stereoselective synthesis of cyclopropane amino acid derivatives. These compounds served as scaffolds for the preparation of a 46-member library. The C-and N-termini of the cyclopropane amino acid derivatives were diversified by condensations with ten amines and ten acylating agents, respectively. To improve yields and accelerate library synthesis, most products were prepared under microwave irradiation and purified by polymer-bound scavengers and SPE methodology. All compounds were analyzed by LC-MS and a representative selection was fully characterized. (c) 2005 Elsevier Ltd. All rights reserved.