Department of Chemistry, University of Kansas, 1251 Wescoe Hall Drive, Lawrence, Kansas 66045, USA.
Org Lett. 2012 Apr 6;14(7):1752-5. doi: 10.1021/ol300352z. Epub 2012 Mar 14.
A highly diastereoselective protocol for the formal nucleophilic substitution of 2-bromocyclopropylcarboxamides with azoles is described. A wide range of azoles, including pyrroles, indoles, benzimidazoles, pyrazoles, and benzotriazoles, can be efficiently employed as pronucleophiles in this transformation, providing expeditious access to N-cyclopropyl heterocycles.
本文描述了一种高非对映选择性的 2-溴环丙基甲酰胺与唑类化合物的亲核取代反应的方法。在这种转化中，可以有效地使用各种唑类化合物，包括吡咯、吲哚、苯并咪唑、吡唑和苯并三唑，作为亲核试剂，为 N-环丙基杂环的快速合成提供了途径。
