An alternative and efficient synthesis of MLN4924, a selective NEDD8 inhibitor

Hong Rae Kim, Young Eum Hyun, Dnyandev B. Jarhad, Jinha Yu, Lak Shin Jeong

Research output: Contribution to journalArticlepeer-review

1 Scopus citations


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 privileged template.

Original languageEnglish
Pages (from-to)2480-2487
Number of pages8
JournalOrganic Chemistry Frontiers
Issue number14
StatePublished - 2019

Bibliographical note

Funding Information:
This work was supported by grants from Mid-career Research Program (2016R1A2B3010164) and the Ministry of Science, ICT & Future Planning (2017M3A9A8032086) of the National Research Foundation (NRF), Korea.

Publisher Copyright:
© the Partner Organisations 2019.


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