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.
描述了通向有价值的
生物活性实体(如
核黄素、
喹唑啉酮和苯二氮卓)的稳健
化学路线。这些路线利用现代流动加氢协议,能够对含有硝基的构筑块进行
化学选择性的还原,从而迅速在原位生成所需的胺中间体。为了利用连续加工的优势,各个步骤被转化为一个串联流动过程,分别以50毫摩尔和120毫摩尔的规模生产选定的苯二氮卓产品。