Optimisation of a Key Cross-coupling Reaction Towards the Synthesis of a Promising Antileishmanial Compound

During the course of a research program aimed at identifying novel antileishmanial compounds, a multi-gram synthesis of -(-4-((4-methoxy-3-(()-3-methylmorpholino)-1-pyrazolo[3,4-]pyrimidin-6-yl)amino)cyclohexyl)-2-methylpropane-1-sulfonamide (( )) was required. This letter describes optimisation of the reaction conditions and protecting group strategy for a key Buchwald-Hartwig coupling, delivering the required quantities of ( ), as well as further compounds in the series.