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02 May 2019

Raul F. Velasco, C├ęsar Guerrero, Gloria Fra, Alejandra Moure, Juan Miguel-Siles, Maria Teresa Quesada-Campos, Jose Ramon Ruiz-Gomez, Ian H. Gilbert, Michael G. Thomas, Timothy J. Miles.

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)-1H-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.