Spirocyclohexadienones and pyrazolines are prevalent core structures in bioactive molecules and natural products. On the other hand,spiro compounds have continued to gain attentions in recent years because of their di...
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Spirocyclohexadienones and pyrazolines are prevalent core structures in bioactive molecules and natural products. On the other hand,spiro compounds have continued to gain attentions in recent years because of their diversified biological activities and pharmacological properties.3 Thus,combining the pyrazolines and cyclohexadienone structural motifs simultaneously into one molecule as spiro-pyrazoline-cyclohexadienones may be significant for drug candidate discovery. Herein,we developed an eficient [3+2] cycloaddition of para-quinone methides and nitrile imines to construct spiro-pyrazoline-cyclohexadienones with high re gio *** p-QMs and nitrile imines bearing electron-donating or electron-withdrawing groups on the phenyl rings were well-tolerated,providing the spiropyyazolines in good to excellent *** straightforward protocol for efficient construction of the privileged spiropyrazolines may be further applied in the pharmaceutical industry and make particularly attractive in organic synthesis.
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