Over the last ten years, there has been a significant advancement in the development of new sulfur-containing compounds used in various industries, such as pharmaceuticals and agriculture. Sulfoximines, sulfonimidoyl fluorides, and sulfonimidamides are types of sulfur-containing chemical compounds with broad potential as therapeutic drugs. However, the synthesis process for these compounds is complex and has limitations.
There are four main chemical approaches commonly used to create sulfoximines, sulfonimidoyl fluorides, and sulfonimidamides. Recently, a new approach called sulfur fluorine exchange (SuFEx) chemistry has gained attention, but it has limitations, such as the requirement for high pressures.
The Moffitt research team aimed to develop a more efficient process for creating sulfoximines, sulfonimidoyl fluorides, and sulfonimidamides. Through various chemical experiments and processes, they developed a reagent called t-BuSF, which serves as a hub in the SuFEx chemical process for synthesizing these sulfur-containing compounds. The use of t-BuSF reduced the number of steps required to make these compounds and improved the reaction times and stability of their chemical precursors.
The researchers further demonstrated the potential utility of t-BuSF in medicinal chemistry in over 70 examples and by preparing five therapeutic targets and intermediates. They showed that t-BuSF was able to create these products in high yields with fewer synthesis steps.
“Given the cost-effectiveness and the chemical space accessible from this reagent platform, it is expected to have positive impacts on the discovery sciences from the development of new medicines and agrochemicals to the discovery of new ligands, organocatalysts, and materials,” said Justin Lopchuk, Ph.D., associate member of the Department of Drug Discovery at Moffitt.
2024-01-22 22:00:05
Link from phys.org
