Biginelli reaction is one of the most remarkable examples of MCRs discovered in 1893 and proof of its importance is the high number of articles reported in the last decade covering this field. This strategy allows the synthesis of important building blocks and versatile synthons such as 3,4-dihydropyrimidin-2-(1H)-one derivatives (DHPMs), which are present motives in organic synthesis owing their biological and pharmacological properties. In this chapter we will cover only some aspects overlooked in the incredible revision performed by Suresh and Sandhu, and reported since 2006. Chiral Lewis and Brønsted acid catalyzed examples, Brønsted base-catalyzed ones, organocatalytic enantioselective Biginelli works or important targets will be disclosed in this interesting chapter.

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