Department of Chemistry, The University of Kansas, 1251 Wescoe Hall Drive, Lawrence, Kansas 66045-75832, USA.
J Org Chem. 2013 Aug 2;78(15):7601-16. doi: 10.1021/jo4011798. Epub 2013 Jul 24.
A highly chemo- and diastereoselective protocol toward amino-substituted donor-acceptor cyclopropanes via the formal nucleophilic displacement in bromocyclopropanes is described. A wide range of N-nucleophiles, including carboxamides, sulfonamides, azoles, and anilines, can be efficiently employed in this transformation, providing expeditious access to stereochemically defined and densely functionalized cyclopropylamine derivatives.
本文描述了一种通过溴代环丙烷中的形式亲核取代反应，高化学选择性和非对映选择性地制备氨基取代给体-受体环丙烷的方法。该转化可以有效地使用各种 N-亲核试剂，包括酰胺、磺酰胺、唑和苯胺，为立体化学确定和高度官能化的环丙胺衍生物提供了快速的合成途径。
