Leibniz-Institut für Katalyse e. V. an der Universität Rostock, Albert-Einstein-Strasse 29a, 18059 Rostock, Germany.
ChemSusChem. 2012 Oct;5(10):2039-44. doi: 10.1002/cssc.201200247. Epub 2012 Aug 14.
A novel catalyst system for efficient amination of allylic alcohols with aryl and alkyl amines is presented. By applying a convenient combination consisting of Pd(OAc)(2)/1,10-phenanthroline, a variety of allylic alcohols reacted smoothly to give the corresponding secondary and tertiary amines in good to excellent yields with high regioselectivity. The usefulness of our protocol is demonstrated in the one-step synthesis of the antifungal drug naftifine and the calcium channel blocker flunarizine.
本文提出了一种新型的用于烯丙醇与芳基和烷基胺高效胺化的催化剂体系。通过应用方便的 Pd(OAc)(2)/1,10-菲咯啉组合，各种烯丙醇反应顺利，以高区域选择性得到相应的仲胺和叔胺，收率良好至优秀。我们的方案在抗真菌药物萘替芬和钙通道阻滞剂氟桂嗪的一步合成中得到了证明。
