Development of an Alternate Synthesis for a Key JAK2 Inhibitor Intermediate via Sequential C–H Bond Functionalization

AN Campbell, KP Cole, JR Martinelli…

Index: Campbell, Alison N.; Cole, Kevin P.; Martinelli, Joseph R.; May, Scott A.; Mitchell, David; Pollock, Patrick M.; Sullivan, Kevin A. Organic Process Research and Development, 2013 , vol. 17, # 2 p. 273 - 281

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Citation Number: 10

Abstract

The development of an alternative synthetic route to a functionalized imidazopyridazine which strategically streamlines the synthesis and avoids a number of problematic reagents is described. Key to the success of this alternative route is the use of two C–H functionalization reactions: a Pd-catalyzed direct benzylation reaction to functionalize a C–H bond with a substituted benzyl group and a V-catalyzed NMO addition reaction to install a ...