Sulfone-substituted Cyclopropanes and Their One-step Synthesis (No. 0128)

 
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Summary

Sulfone-substituted cyclopropanes having potential drug design applications.

The global drug discovery market continues to have strong growth around the world. In this market, the cyclopropane motif is present in a variety of bioactive natural products and medicinally important molecules. However, normally, the synthesis of cyclopropanes needs multiple steps, resulting in lower yields with a greater amount of waste. Especially, sulfone substituted cyclopropanes are difficult to synthesize and almost not commercially available. Here, we present a promising synthesis method developed by a group of researchers led by Dr. Eugene Khaskin. The developed technology overcomes the above problems and provides a short and simple 1-step method unlocking new cyclopropanes.

 

Lead Researcher:
Eugene Khaskin

Science and Technology Group

Applications

  • Drug Design
  • Drug Discovery

 

Advantages

  • 3-component reaction in 1-step
  • High diastereoselectivity
  • Simple and cheap starting materials (alcohol, ester)

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Technology's Essence

Essentially, Dr. Eugene Khaskin has developed a novel chemically and biologically important sulfone-substituted cyclopropane synthesis method. The technology enables the synthesis of sulfonated cyclopropanes via a Ru(II)-catalyst with 3 alcohol/ester components. Furthermore, this technology can control the placement of substituents on the cyclopropane for specific designs.

 

Media Coverage and Presentations

 JST Technology Showcase Presentation

 

CONTACT FOR MORE INFORMATION

  Graham Garner
Technology Licensing Section

  tls@oist.jp
  +81(0)98-966-8937