Wang Tammy, Magnin David R, Hamann Lawrence G
Department of Metabolic Diseases Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, P.O. Box 5400, Princeton, New Jersey 08543-5400, USA.
Org Lett. 2003 Mar 20;5(6):897-900. doi: 10.1021/ol034072h.
[reaction: see text] 1-Aminonaphthalenes and 5- and 8-aminoquinolines were rapidly prepared from the respective aryl bromides in good yields by Pd-catalyzed aryl amination under microwave conditions. Consistent improvements in yields over those obtained under standard conditions were seen with quinoline substrates. In the cases where 5-bromo-8-cyanoquinoline was used as a substrate, no desired products were obtained under standard conditions with a number of different primary and secondary amines. However, microwave conditions provided the desired products in good to excellent yields.
[反应：见正文] 在微波条件下，通过钯催化的芳基胺化反应，可从相应的芳基溴化物中快速制备1-氨基萘以及5-和8-氨基喹啉，产率良好。对于喹啉底物，与标准条件下获得的产率相比，产率持续提高。在使用5-溴-8-氰基喹啉作为底物的情况下，在标准条件下与多种不同的伯胺和仲胺反应时，未得到所需产物。然而，微波条件下能以良好至优异的产率得到所需产物。
