Modification of Boc-Protected CAN508 via Acylation and Suzuki-Miyaura Coupling.

The cyclin-dependent kinase inhibitor, CAN508, was protected with di--butyl dicarbonate to access the amino-benzoylated pyrazoles. The bromo derivatives were further arylated by Suzuki-Miyaura coupling using the XPhos Pd G2 pre-catalyst. The coupling reaction provided generally the -substituted benzoylpyrazoles in the higher yields than the -substituted ones.