Sulfone-substituted cyclopropanes have potential drug design applications.
Abstract
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.
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.
Applications
- Drug Design
- Drug Discovery
Advantages
- 3-component reaction in 1-step
- High diastereoselectivity
- Simple and cheap starting materials (alcohol, ester)
Website