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Xanthenes are a class of natural and synthetic heterocyclic compounds that exhibit a broad spectrum of biological properties and synthetic applications.

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A new series of bis‐heteroarylaminomethylnaphthoquinone Mannich bases have been synthesized through facial and efficient one‐pot pseudo five‐component reactions of lawsone, different heteroaryl amines and terephthaldehyde using p‐TSA as catalyst in CH3CN under reflux conditions. The high yields of products, very simple operation, readily available starting materials, high atom‐economy, easy workup procedure and isolation/purification of target products without chromatography are the main benefits of this synthetic strategy.

4-Aminocoumarins represent an important class of a versatile scaffold in organic synthesis and have been consistently used as a building block in organic chemistry for the synthesis of different heterocyclic compounds.