Zhejiang Province Key Laboratory of Anti-Cancer Drug Research, College of Pharmaceutical Science, Zhejiang University , Hangzhou 310058, P. R. China.
Org Lett. 2013 Dec 6;15(23):5967-9. doi: 10.1021/ol402810f. Epub 2013 Nov 20.
A simple, multicomponent, and straightforward reaction of vinyl azide, aldehyde, and tosylhydrazine affords the construction of 3,4,5-trisubstituted 1H-pyrazoles regioselectively in the presence of base with moderate to excellent yields. A range of functionality could be tolerated in this methodology, and a possible mechanism is proposed.
在碱存在下,乙烯基叠氮化物、醛和对甲苯磺酰肼发生简单、多组分、直接的反应,可在中等至优异的产率条件下区域选择性地构建 3,4,5-三取代的 1H-吡唑。该方法可耐受多种官能团,提出了一种可能的反应机理。