Zeolite catalyzed solvent-free one-pot synthesis of dihydropyrimidin-2(1H)-ones – A practical synthesis of monastrol
2009

Synthesis of Dihydropyrimidin-2(1H)-ones Using Zeolite

publication Evidence: moderate

Author Information

Author(s): Kulkarni Mukund G, Chavhan Sanjay W, Shinde Mahadev P, Gaikwad Dnyaneshwar D, Borhade Ajit S, Dhondge Attrimuni P, Shaikh Yunnus B, Ningdale Vijay B, Desai Mayur P, Birhade Deekshaputra R, Clayden Jonathan

Primary Institution: Department of Chemistry, University of Pune

Hypothesis

Can zeolite catalyze a solvent-free one-pot synthesis of dihydropyrimidin-2(1H)-ones?

Conclusion

The study successfully developed a practical methodology for synthesizing dihydropyrimidones with high yields using zeolite as a catalyst.

Supporting Evidence

  • The zeolite catalyst was recyclable and could be reused multiple times without loss of yield.
  • The synthesis method was effective for both aliphatic and aromatic aldehydes.
  • Monastrol, a potent inhibitor of kinesin Eg5, was synthesized with a yield of 94%.
  • The reaction can be scaled up to produce larger quantities of the product.

Takeaway

This study shows how to make a special chemical called dihydropyrimidin-2(1H)-ones using a simple method that doesn't need any solvents.

Methodology

A one-pot synthesis using a catalytic amount of zeolite under solvent-free conditions.

Limitations

The reaction yields were low when using certain substituted aldehydes.

Digital Object Identifier (DOI)

10.3762/bjoc.5.4

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