Improved Synthetic Route and Scale-Up of GSK973 using SiliaMetS Thiol for Pd Scavenging

The bromo- and extra-terminal domain (BET) family of proteins is known to play a major role in the regulation of gene transcription. An intense area of research is now using BET inhibitors for possible cancer treatment, and their therapeutic effects are being investigated. GSK973 is one such inhibitor, needed in larger quantities for pre-clinical efficacy and safety studies for oncology trials. By working on improving the synthetic route for its large-scale synthesis, the team at GSK included a purification step using SiliaMetS Thiol for the removal of the residual Pd catalyst.
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