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Metal-Free Synthesis of Pyrazoles from 1,3-Diarylpropenes and Hydrazines via Multiple Inter-/Intramolecular C–H Aminations
Tang, Li,Ma, Minyan,Zhang, Qi,Luo, Huan,Wang, Tao,Chai, Yonghai
, p. 2610 - 2620 (2017)
A facile and metal-free access to pyrazoles from 1,3-diarylpropenes and hydrazines via multiple inter-/intramolecular C-H aminations was described. Under the neutral and mild 2,3-dichloro-5,6-dicyanobenzoquinone (DDQ) oxidative conditions, various disubstituted pyrazoles were synthesized in moderate to excellent yields. This method provides a pot- and step-economic strategy for the construction of pyrazoles, especially those for drug discovery. (Figure presented.).