Chemists develop faster way to modify drug molecules using fluorine compounds
Researchers have created a simpler method to chemically transform trifluoromethyl compounds into useful building blocks for pharmaceuticals. The technique works faster, requires fewer toxic chemical odors, and already works on existing drugs like celecoxib, potentially accelerating drug development and reducing manufacturing costs.
Originaltitel: Defluorinative thio-functionalization: direct synthesis of methyl-dithioesters from trifluoromethylarenes
<p>A new functional group transformation allowing the synthesis of methyl-dithioesters from readily available trifluoromethyl arenes via defluorinative functionalization has been developed. This microwave-assisted method is operationally simple, rapid, and eliminates the need for pre-functionalization while accommodating a broad range of functional groups. In addition, it does not rely on highly odorous thiol sources, and utilizes the commercially available reagent BF3SMe2 complex as a multifunctional Lewis acid/sulfur source/defluorination and demethylation agent. Finally, this approach is suitable for late-stage functionalizations, as shown by the transformation of pharmaceuticals leflunomide, flufenamic acid and celecoxib into novel methyl-dithioester derivatives.</p>