State Key Laboratory of Medicinal Chemical Biology and College of Pharmacy, Nankai University, Tianjin 300071, PR China.
Org Lett. 2013 Jan 4;15(1):18-21. doi: 10.1021/ol3028708. Epub 2012 Dec 14.
A facile approach to the diazotransfer reagent of imidazole-1-sulfonyl azide was reported. The procedure was well optimized to clarify potential explosion risks. A high production yield as well as small batch variation was achieved even without careful pretreatment of reagents and solvents. HPLC and NMR methods to monitor the process were provided. These features made this protocol suitable for large scale preparation in academia and industry as well.
报道了一种咪唑-1-磺酰基叠氮的重氮转移试剂的简便方法。该方法经过了很好的优化，以澄清潜在的爆炸风险。即使不对试剂和溶剂进行仔细预处理，也能获得高产率和较小的批间变化。提供了用于监测该过程的 HPLC 和 NMR 方法。这些特点使得该方案适用于学术界和工业界的大规模制备。
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