School of Chemistry and Molecular Engineering, East China University of Science and Technology, Shanghai, 200237, China.
Molecules. 2012 Apr 16;17(4):4533-44. doi: 10.3390/molecules17044533.
Chlorination with equimolar POCl₃ can be efficiently achieved not only for hydroxypyrimidines, but also for many other substrates such as 2-hydroxy-pyridines, -quinoxalines, or even -amides. The procedure is solvent-free and involves heating in a sealed reactor at high temperatures using one equivalent of pyridine as base. It is suitable for large scale (multigram) batch preparations.
用等摩尔的 POCl₃进行氯化不仅可以有效地实现羟嘧啶,还可以实现许多其他底物,如 2-羟基吡啶、-喹喔啉,甚至 -酰胺。该过程是无溶剂的,并且涉及在密封反应器中使用吡啶作为碱在高温下加热,使用一个当量。它适用于大规模(多克)批量制备。