A novel approach for the synthesis of regioselective pyrano [3,4-b]quinolines from 3-alkynylquinoline aldehydes with alcohols as nucleophiles has been elucidated. This protocol has shown high generality of functional group and provides the pyrano-annulated products good to excellent yields. This methodology was adopted a new synthetic strategy to develop the 3-alkynylquinolinealdehydes by using methanol as a C1 source.
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