Csajági Csaba, Borcsek Bernadett, Niesz Krisztián, Kovács Ildikó, Székelyhidi Zsolt, Bajkó Zoltán, Urge László, Darvas Ferenc
ThalesNano Inc., Záhony u. 7., Budapest, Hungary.
Org Lett. 2008 Apr 17;10(8):1589-92. doi: 10.1021/ol7030894. Epub 2008 Mar 22.
Halogenated aryl carboxylic acids were efficiently converted to the corresponding dicarboxylic acid monoamides by a one-step Pd-catalyzed aminocarbonylation in a micro/meso fluidic continuous flow reactor (X-Cube) operated at high pressure and high temperature with CO gas introduction. Reaction parameters (solvent, base, catalyst, pressure, temperature) were rapidly optimized in the reactions, which required less than 2 min. The method gave improved results over comparable batch techniques and is also suited to automated parallel syntheses of compound libraries.
在配备有CO气体引入装置的微/介观流体连续流动反应器（X-Cube）中，通过一步钯催化的氨羰基化反应，卤代芳基羧酸能高效地转化为相应的二羧酸单酰胺。该反应在高压和高温下进行。反应参数（溶剂、碱、催化剂、压力、温度）能在不到2分钟的反应中迅速得到优化。与类似的间歇技术相比，该方法取得了更好的结果，并且也适用于化合物库的自动化平行合成。
