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The Aldehyde–Amine–Alkyne reaction (A3) proves to be a powerful methodology as a coupling step of the Build/Couple/Pair approach in Diversity Oriented Synthesis (DOS) because it can lead to the formation of polyfunctionalized intermediates suitable for the creation of different molecular entities. In this work we used cyclic α‐amino aldehyde moieties for the microwave‐assisted A3 coupling reaction,...
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