Chemical Methodologies and Library Development Center, University of Kansas, Delbert M. Shankel Structural Biology Center, West Campus, Lawrence, 66047, USA.
Angew Chem Int Ed Engl. 2011 Mar 14;50(12):2734-7. doi: 10.1002/anie.201007133. Epub 2011 Feb 23.
Minimization of 1,3-allylic strain is a recurring element in the design of a stereochemically- and spatially-diverse collection of 2-arylpiperidines. Here, stereochemically-diverse scaffolding is first constructed using A strain to guide the regioselective addition of nucleophiles, which serve as handles for further substitution. -substitution with alkyl and acyl substituents again leverages A strain to direct each stereoisomer to two different conformer populations, doubling the number of library members.
最小化 1,3-烯丙基应变是设计具有立体化学和空间多样性的 2-芳基哌啶化合物库的常用方法。在此，首先使用 A 应变构建立体化学多样化的支架，以引导亲核试剂的区域选择性加成，亲核试剂作为进一步取代的反应点。-用烷基和酰基取代基取代再次利用 A 应变将每个立体异构体引导到两个不同的构象群体，使库成员数增加一倍。
