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

Tetrahedron Lett 2019 May;60(18):1243-1247

Global Health R&D, GlaxoSmithKline, Calle Severo Ochoa, 2, 28760, Tres Cantos, Madrid, Spain.

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.

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http://dx.doi.org/10.1016/j.tetlet.2019.03.068DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6480136PMC
May 2019
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