Pharmaceuticals derivatives of 3,4-dihydropyrimidin-2(1H)-ones/thiones have many applications in the medical field including, anticancer, antiviral, and calcium channel inhibition activities. The synthesis of these compounds is achieved via the Biginelli reaction which involves the combination of aldehydes, 1,3-dicarbonyl compounds, and (thio)urea. The Biginelli reaction is tolerant of a wide diversity in reactants electronic and steric structures.  However, even though the Biginelli reaction is tolerant of a wide diversity of reactants, the utility of the reaction can be impacted by changes to the electronic and steric changes while corresponding yields and reaction times vary.  Can a procedure for the Biginelli reaction be developed that allows for the efficient and high yielding synthesis of 3,4-dihydropyrimidin-2(1H)-ones/thiones? <br/>            Recently, we have developed a method for the direct coupling of the amine and carboxylic acid using nano-reactors. Nano-reactors have four characteristics that allow it to facilitate direct amide bond coupling: (1) Nano-reactors absorb organic molecules into central cavities. (2) Upon absorption of organic molecules, the nano-reactor swells 3-5 times its dry volume. (3) Upon removal of organic molecules, the nano-reactor assumes its original dry volume. (4) The nano-reactor is hydrophobic, water does not enter the central cavity and water synthesized in the cavity migrates out of the cavity.<br/>            The authors present the development of a new, efficient, and high yielding procedure for the synthesis of 3,4-dihydropyrimidin-2(1H)-ones/thiones and its application to the synthesis of pharmaceuticals.<br/>

Efficient and complete synthesis of 3,4-dihydropyrimidin-2(1H)-ones/thiones for pharmaceutical applications using nano-reactors

2019 Spring National Meeting

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