Novartis Institute for BioMedical Research, Forum 1, 4056 Basel, Switzerland.
Org Lett. 2011 Jan 21;13(2):320-3. doi: 10.1021/ol1027927. Epub 2010 Dec 16.
A flow method for the synthesis of aliphatic and aromatic diazoketones from acyl chloride precursors has been developed and used to prepare quinoxalines in a multistep sequence without isolation of the potentially explosive diazoketone. The protocol showcases an efficient in-line purification using supported scavengers with time-saving and safety benefits and in particular a reduction in the operator's exposure to carcinogenic phenylenediamines.
已开发出一种从酰氯前体制备脂肪族和芳香族重氮酮的流动方法,并将其用于多步序列中制备喹喔啉,而无需分离潜在爆炸的重氮酮。该方案展示了使用支持的清除剂进行高效的在线纯化,具有节省时间和安全的优点,特别是减少了操作人员接触致癌性苯二胺的机会。