通过基于化学选择性流动氢化反应合成核黄素、喹喔啉酮和苯二氮䓬类化合物。

Baumann Marcus, Baxendale Ian R, Hornung Christian H, Ley Steven V, Rojo Maria Victoria, Roper Kimberley A

Department of Chemistry, University of Durham, South Road, Durham DH1 3LE, UK.

Department of Chemistry, University of Cambridge, Lensfield Road, Cambridge CB2 1EW, UK.

Molecules. 2014 Jul 8;19(7):9736-59. doi: 10.3390/molecules19079736.

Robust chemical routes towards valuable bioactive entities such as riboflavines, quinoxalinones and benzodiazepines are described. These make use of modern flow hydrogenation protocols enabling the chemoselective reduction of nitro group containing building blocks in order to rapidly generate the desired amine intermediates in situ. In order to exploit the benefits of continuous processing the individual steps were transformed into a telescoped flow process delivering selected benzodiazepine products on scales of 50 mmol and 120 mmol respectively.

描述了通往有价值的生物活性物质（如核黄素、喹喔啉酮和苯二氮䓬）的稳健化学路线。这些路线利用现代流动氢化协议，能够对含硝基的结构单元进行化学选择性还原，以便原位快速生成所需的胺中间体。为了利用连续加工的优势，将各个步骤转化为一种串联流动过程，分别以50 mmol和120 mmol的规模生产选定的苯二氮䓬产品。