Optimisation of a key cross-coupling reaction towards the synthesis of a promising antileishmanial compound

Abstract During the course of a research program aimed at identifying novel antileishmanial compounds, a multi-gram synthesis of N -( trans -4-((4-methoxy-3-(( R )-3-methylmorpholino)-1 H -pyrazolo[3,4- d ]pyrimidin-6-yl)amino)cyclohexyl)-2-methylpropane-1-sulfonamide (( R ) -1 ) 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 ( R ) -1 , as well as further compounds in the series.