1. Practical gram-scale synthesis of bicyclol metabolites M2 and M3.
- Author
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Ma, Bo, Wang, Zhen-Wei, Liu, Xiao-Yu, Wang, Mi-Juan, Zhang, Yong-Wang, Zhang, Meng, Jiao, Xiao-Zhen, and Xie, Ping
- Subjects
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PATIENT safety , *NUCLEAR magnetic resonance spectroscopy , *BIPHENYL compounds , *METABOLITES , *HEPATITIS B , *DRUG efficacy , *DRUG interactions , *MOLECULAR structure , *MASS spectrometry , *DEMETHYLATION , *CHROMATOGRAPHIC analysis - Abstract
Bicyclol, an innovative hepatoprotective drug, was approved by the Chinese National Medical Products Administration (NMPA) in 2001 to treat Hepatitis B and drug-induced liver injury. Two active metabolites of bicyclol have been identified as M2 and M3. To evaluate the impact on drug safety and efficacy of possible drug-drug interactions (DDIs) associated with these metabolites, a sufficient quantity of these metabolites is required. Herein, we report a concise novel route for the synthesis of M2 and M3 using the Suzuki-Miyaura coupling as the key step. Furthermore, we complete the gram-scale syntheses of M2 and M3. [ABSTRACT FROM AUTHOR]
- Published
- 2024
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