Institute for Organic Chemistry, Saarland University, Saarbruecken, Germany.
Org Biomol Chem. 2012 Oct 3;10(41):8268-75. doi: 10.1039/c2ob26351c.
Pd-catalyzed allylations are excellent tools for stereoselective peptide modifications, showing several advantages compared to normal alkylations. Reactions of internal peptide amide enolates with Pd-allyl complexes proceed not only with high yields of up to 86%, they show also high regio- and diastereoselectivities (88-99%), giving rise to the trans-configured products. Therefore, this protocol is a powerful synthetic tool for the synthesis of natural product and drug molecules.
Pd 催化的烯丙基化反应是立体选择性肽修饰的优秀工具，与普通的烷基化反应相比具有多项优势。Pd-烯丙基配合物与内部肽酰胺烯醇化物的反应不仅产率高达 86%，而且具有很高的区域和立体选择性（88-99%），生成反式构型产物。因此，该方案是合成天然产物和药物分子的有力合成工具。
