Abstract
o-Alkynylaryl 2-cyanoacrylates have been disclosed as a new synthon for the regioselective synthesis of isoquinolones and naphthyridinones under mild reaction conditions. The attractive feature of this investigation includes carbon-carbon double bond cleavage under metal-free conditions by an intramolecular SN2 reaction. Incorporating two distinct C-I bonds in the resulting products provides facile opportunity for structural elaboration. The viability of the present protocol was unveiled by postfunctionalization with drug analogues and gram-scale synthesis.
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