CVMED Medicinal Chemistry, Pfizer Inc., Eastern Point Road, Groton, Connecticut 06340, United States.
Org Lett. 2010 Nov 19;12(22):5254-7. doi: 10.1021/ol102301u. Epub 2010 Oct 19.
A general and facile one-pot amination procedure for the synthesis of 2-aminopyridines from the corresponding pyridine-N-oxides is presented as a mild alternative to S(N)Ar chemistry. A variety of amines and heterocyclic-N-oxides participate effectively in this transformation which uses the phosphonium salt, PyBroP, as a means of substrate activation.
本文提出了一种通用且简便的一锅法胺化反应,可从相应的吡啶-N-氧化物合成 2-氨基吡啶,是 S(N)Ar 化学的温和替代方法。各种胺和杂环-N-氧化物均可有效地参与此转化,其中使用磷鎓盐 PyBroP 作为底物活化剂。