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First, a 1,3-dipolar cycloaddition will be used to selectively combine the azide and alkyne functionalities of these tripeptides, thus generating the desired macrocyclic peptidomimetic architecture. Intramolecular cyclization reactions between amine and carbonyl moieties would then introduce the DKP motif into the macrocyclic framework.There are several key synthetic challenges associated with the proposed route. Two are particularly worthy of note. First, epimerization of the chiral centers needs to be avoided at all stages of the synthesis in order to obtain the products as single stereoisomers (and thus access the full matrix of stereochemical isomers in the library, i.e., maximizing stereochemical diversity). In addition, generation of both 1,4- and 1,5-subsituted triazoles from each tripetide derivative is desired so as to be able to access the desired scaffold diversity in the library; thus the 1,3-dipolar cycloaddition needs to operate in a highly controllable and regioselective fashion. |
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铁杆木虫 (著名写手)
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爱与雨下(金币+1): ！！~~ 2011-08-26 15:16:09
雨菲9323(金币+20, 翻译EPI+1): 谢谢 2011-08-26 16:24:04
爱与雨下(金币+1): ！！~~ 2011-08-26 15:16:09
雨菲9323(金币+20, 翻译EPI+1): 谢谢 2011-08-26 16:24:04
| 首先，1，3偶极环加成被用来选择性的将这些三肽的azide和alkyne的功能性集团结合。因此，可以得到期望的大环多肽模拟分子结构体系。胺和羰基结构的分子内环化反应可以进一步的将DKP模型引入到大环的框架中。合成路线中还有一些关键的合成挑战。有两点需要值得注意。首先，为了获得单一手性的目标产物，手性中心的异构化需要在所有的合成步骤中避免（通过立体化学异构体库的矩阵来最大化立体化学多样性）。然后，从每个三肽衍生产生1,4-，1,5-取代的三唑是所期望的，从此能够来获得所期望的骨架多样的分子库。因此，1,3偶极环加成的操作需要在高度可控的区域选择方式。 |
2楼2011-08-26 15:14:11
