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An Alternative and Efficient Synthesis of MLN4924, A Selective NEDD8 Inhibitor

Abstract

An efficient synthesis of MLN4924, a small molecule inhibitor of NEDD8-activating enzyme (NAE) in clinical trial as an anticancer agent, has been accomplished via regioselective α-alkoxy removal by Al(Hg) and stereoselective reduction based on the conformational study as key steps. The present synthesis was achieved through a versatile cyclopentanone intermediate, which is expected to provide an easy access to structural analogues of MLN4924 for further exploration as a biologically previleged template.

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Publication details

The article was received on 15 Apr 2019, accepted on 10 May 2019 and first published on 13 May 2019


Article type: Research Article
DOI: 10.1039/C9QO00507B
Org. Chem. Front., 2019, Accepted Manuscript

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    An Alternative and Efficient Synthesis of MLN4924, A Selective NEDD8 Inhibitor

    H. Kim, Y. E. Hyun, D. Jarhad, J. Yu and L. S. Jeong, Org. Chem. Front., 2019, Accepted Manuscript , DOI: 10.1039/C9QO00507B

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