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Citation: Fan Lingling, Luo Zhongfu, Luo Bilan, Tang Lei, Li Yong. Optimization of Synthetic Process for the CRBN Regulator Avadomide[J]. Chemistry, ;2019, 82(9): 837-841. shu

Optimization of Synthetic Process for the CRBN Regulator Avadomide

College of Pharmacy, Guizhou Medical University, Guiyang 550025

Corresponding author: Li Yong, liyong19851016@126.com
Received Date: 26 June 2019
Accepted Date: 18 July 2019

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Avadomide is a potential drug for the treatment of advanced solid tumors, which is in phase Ⅱ clinical trials. In this work, the synthetic process of Avadomide was optimized and improved. Using 3-nitrophthalimide as the starting material, Avadomide was obtained by ring-cleavage, Hoffman degradation, cyclization, ester aminolysis reaction and Pd(OH)₂/C hydrogenation reduction. The overall yield was 46.9%, and the target compound was identified by ¹H NMR, ¹³C NMR and HRMS, whose purity was 99.5% through HPLC test. In comparison with literature methods, this synthetic route has the advantages of mild reaction conditions, simple post-treatment, high yield and easy work-up, so it is suitable for industrial production of Avadomide.
- CRBN regulator,
- Avadomide,
- Process optimization
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