Identification of 6-amino-1-pyrazolo[3,4-]pyrimidines with efficacy against visceral leishmaniasis.

Visceral leishmaniasis (VL) affects millions of people across the world, largely in developing nations. It is fatal if left untreated and the current treatments are inadequate. As such, there is an urgent need for new, improved medicines.

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.