Asymmetric Synthesis of Fluoro-MLN4924 as a Selective NEDD8-Activating Enzyme (NAE) Inhibitor

Hong Rae Kim, Dnyandev B. Jarhad, Pramod K. Sahu, Kisu Sung, Dayoung An, Young Eum Hyun, Jinha Yu, Lak Shin Jeong

Research output: Contribution to journalArticlepeer-review

Abstract

Based on bioisosteric rationale, fluorinated analogues of MLN4924, which is a selective NEDD8-activating enzyme inhibitor, were designed and their asymmetric syntheses were accomplished via stereoselective reduction, regioselective isopropylidene cleavage and diethylaminosulfur trifluoride (DAST) fluorination as key steps.

Original languageEnglish
Pages (from-to)1641-1647
Number of pages7
JournalAsian Journal of Organic Chemistry
Volume8
Issue number9
DOIs
StatePublished - 1 Sep 2019

Keywords

  • Bioisotere
  • DAST fluorination
  • Fluoro-MLN4924
  • MLN4924
  • NEDD8 inhibitor

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