Annulative Tandem Reactions Based on Pd0/tBu3P-Catalyzed Cross-Coupling and C(sp3)[BOND]H Bond Activation


  • We thank the NIH (GM69704) for funding. Partial support from the PSC-CUNY Research Award Program is gratefully acknowledged. We thank Ms. Hui-Yu Liu and Ms. Anna P. Yeung for some experimental work, Prof. Shuiqin Zhou for helpful discussions, and Prof. Alec Greer for help with the GCMS analysis.


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All together now: Pd0/tBu3P-catalyzed annulative tandem reactions of 1,2-dihalobenzenes were carried out with hindered Grignard reagents. This new type of tandem reaction is believed to occur through cross-coupling followed by cyclization with C(sp3)[BOND]H bond activation as the key step and allows one-step access to potentially useful substituted fluorenes in high yield from readily available 1,2-dibromobenzenes and 1-bromo-2-iodobenzene.