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 language | English |
|---|---|
| Pages (from-to) | 1641-1647 |
| Number of pages | 7 |
| Journal | Asian Journal of Organic Chemistry |
| Volume | 8 |
| Issue number | 9 |
| DOIs | |
| State | Published - 1 Sep 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.
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:
© 2019 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim
Keywords
- Bioisotere
- DAST fluorination
- Fluoro-MLN4924
- MLN4924
- NEDD8 inhibitor
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