A practical synthesis of YZD-7082B, a novel orally bioavailable selective estrogen receptor degrader (SERD) for the treatment of ER plus breast cancer
文献类型：期刊论文
| 作者 | He, Yongqi1,2; Leng, Xin-Yu1,3; Wang, Runying1,3; Sun, Lulu1; Zhang, Dan1; Yang, Yushe1,2,3
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| 刊名 | MOLECULAR DIVERSITY
 |
| 出版日期 | 2025-03-16 |
| 页码 | 12 |
| 关键词 | Suzuki coupling Hydrogenation Chiral resolution Reduction of amide Recrystallization |
| ISSN号 | 1381-1991 |
| DOI | 10.1007/s11030-025-11154-1 |
| 英文摘要 | In previous studies, we discovered YZD-7082B, a selective estrogen receptor degrader (SERD) with excellent comprehensive properties. Here, we reported the development of an efficient multigram-scale synthetic process for YZD-7082 in 13 steps. The route featured a chiral resolution of a thiochroman intermediate with a unique cis-1,2-diaryl motif using a chiral amine and a mild reduction of amide using ZnEt2/LiCl/(EtO)(3)SiH system. This approach also overcomes the issues of high loadings of palladium catalysts and long reaction time. The developed process provided YZD-7082B with an HPLC purity of > 99.8% and ee of > 99%. |
| WOS关键词 | REDUCTION ; AMIDES ; SECONDARY |
| 资助项目 | Youth Innovation Promotion Association of Chinese Academy of Sciences[2021275] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Chemistry ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:001446044900001 |
| 出版者 | SPRINGER |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/316650]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Zhang, Dan; Yang, Yushe |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China 2.Nanjing Univ Chinese Med, Sch Chinese Mat Med, Nanjing 210023, Peoples R China 3.Univ Chinese Acad Sci, Sch Pharm, Beijing 100049, Peoples R China |
| 推荐引用方式 GB/T 7714 | He, Yongqi,Leng, Xin-Yu,Wang, Runying,et al. A practical synthesis of YZD-7082B, a novel orally bioavailable selective estrogen receptor degrader (SERD) for the treatment of ER plus breast cancer[J]. MOLECULAR DIVERSITY,2025:12. |
| APA | He, Yongqi,Leng, Xin-Yu,Wang, Runying,Sun, Lulu,Zhang, Dan,&Yang, Yushe.(2025).A practical synthesis of YZD-7082B, a novel orally bioavailable selective estrogen receptor degrader (SERD) for the treatment of ER plus breast cancer.MOLECULAR DIVERSITY,12. |
| MLA | He, Yongqi,et al."A practical synthesis of YZD-7082B, a novel orally bioavailable selective estrogen receptor degrader (SERD) for the treatment of ER plus breast cancer".MOLECULAR DIVERSITY (2025):12. |
入库方式： OAI收割
来源：上海药物研究所
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