Weigand Klaus, Pelka Sylvie
Novartis Research Institute, Medicinal Chemistry Unit, Brunner Strasse 59, A-1235 Vienna, Austria.
Mol Divers. 2003;7(2-4):181-4. doi: 10.1023/b:modi.0000006821.42063.6b.
In this study, the microwave-assisted Pd(0)-catalyzed coupling of aryl halides to Rink resins is compared to a conventional heating protocol. While yields and purities of the coupling products were comparable under both conditions, microwave heating allows a significant acceleration of the reaction. The coupling of electron-deficient aryl halides proceeded within 10-15 minutes, while under conventional conditions 20 h of heating were necessary for complete conversion.
在本研究中,将微波辅助的芳基卤化物与Rink树脂的钯(0)催化偶联反应与传统加热方法进行了比较。虽然在两种条件下偶联产物的产率和纯度相当,但微波加热能显著加快反应速度。缺电子芳基卤化物的偶联反应在10 - 15分钟内即可完成,而在传统条件下则需要20小时加热才能完全转化。