This method demonstrates regioselective cyclization in alkynyl-tethered arenes, suggesting improved yields and selectivity.
Herein, we report palladium(II) and BF3·OEt2 cooperatively catalyzed regioselective ipso-cyclization of alkynyl-tethered para-methoxylated arenes and ortho-cyclization of alkynyl-tethered arenes to prepare spiropyrrolo[2,1-b]quinazolinone-cyclohexadienones and 2,3-fused quinazolinones in good to excellent yields with high regioselectivity, respectively. DFT calculations revealed that the self-assembly of hydrogen-bonding between OAc anion and hydrogen atom of terminal alkyne facilitated ipso-cyclization for the para-methoxy group on the N-aryl moieties. The present method features broad substrate scope, palladacycle as the real catalyst, and hydrogen-bonding enhanced regioselective hydroarylation cyclization.
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Wang et al. (2025) studied this question.
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