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.
Applications
- Drug Design
- Drug Discovery
Advantages
- 3-component reaction in 1-step
- High diastereoselectivity
- Simple and cheap starting materials (alcohol, ester)
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