Process Development and GMP Production of a Potent NAE Inhibitor Pevonedistat

I Armitage, EL Elliott, F Hicks, M Langston…

Index: Armitage, Ian; Berne, Alexander M.; Elliott, Eric L.; Fu, Mingkun; Hicks, Frederick; McCubbin, Quentin; Zhu, Lei Organic Letters, 2012 , vol. 14, # 10 p. 2626 - 2629

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Abstract

A practical synthesis of a novel NEDD8-activating enzyme (NAE) inhibitor pevonedistat (MLN4924) is described. Key steps include an enantioselective synthesis of an amino-diol cyclopentane intermediate containing three chiral centers and a novel, regioselective

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