A new strategy for the construction
of two kinds of fully substituted
pyrroles, including 2-aminopyrroles and bicyclic pyrroles from Morita–Baylis–Hillman
(MBH) acetates with 1,1-enediamines (EDAMs), or heterocyclic ketene
aminals (HKAs) via base-promoted tandem Michael addition, elimination,
and aromatization sequence has been developed, affording the expected
products in moderate to excellent yields. This methodology is a highly
efficient, concise way to access 2-aminopyrroles or bicyclic pyrroles
with diversity in molecular structures from accessible building blocks
under moderate reaction conditions.
An efficient strategy for the synthesis of substituted bicyclic 2-pyridones is developed. The proposed approach is based on the regioselective N-acylation of heterocyclic ketene aminals (HKAs) with methacrylic anhydride or crotonic anhydride.
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