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

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)