Practical gram-scale synthesis of bicyclol metabolites M2 and M3

被引：1

作者：

Ma, Bo ^{[1
]}

Wang, Zhen-Wei ^{[1
]}

Liu, Xiao-Yu ^{[1
]}

Wang, Mi-Juan ^{[2
]}

Zhang, Yong-Wang ^{[2
]}

Zhang, Meng ^{[2
]}

Jiao, Xiao-Zhen ^{[1
]}

Xie, Ping ^{[1
]}

机构：

[1] Chinese Acad Med Sci & Peking Union Med Coll, Inst Mat Med, State Key Lab Bioact Subst & Funct Nat Med, Beijing Key Lab Act Subst Discovery & Druggabil Ev, Beijing 100050, Peoples R China

[2] Beijing Union Pharmaceut Factory Ltd, Beijing 102600, Peoples R China

来源：

JOURNAL OF ASIAN NATURAL PRODUCTS RESEARCH | 2024年 / 26卷 / 03期

关键词：

Bicyclol; metabolites; gram-scale synthesis; Suzuki-Miyaura coupling; DEMETHYLATION; MECHANISM;

D O I：

10.1080/10286020.2023.2270440

中图分类号：

Q94 [植物学];

学科分类号：

071001 ;

摘要：

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.

引用

页码：342 / 352

页数：11

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