选择性雌激素受体降解剂(S)-8-(4-(1-(3-氟丙基)吡咯烷-3-基)氧基)苯基)-7-(4-羟基苯基)-5,6-二氢萘-2-醇的汇聚合成
收稿日期: 2024-03-06
修回日期: 2024-05-21
网络出版日期: 2024-06-24
基金资助
南京医科大学科技发展基金(NMUB20210013); 南京医科大学内涵建设重点项目; 中国博士后科学基金(2022M711419); 及江苏省自然科学基金(BK20231266)
Convergent Strategy to Synthesize (S)-8-(4-((1-(3-Fluoropropyl)-pyrrolidin-3-yl)oxy)phenyl)-7-(4-hydroxyphenyl)-5,6-dihydronaphthalen-2-ol as a Selective Estrogen Receptor Degrader
Received date: 2024-03-06
Revised date: 2024-05-21
Online published: 2024-06-24
Supported by
Science and Technology Development Foundation of Nanjing Medical University(NMUB20210013); Key Project of Connotation Construction of Nanjing Medical University; China Postdoctoral Science Foundation(2022M711419); Natural Science Foundation of Jiangsu Province(BK20231266)
报道了一种更为可行的选择性雌激素受体降解剂(S)-8-(4-(1-(3-氟丙基)吡咯烷-3-基)氧)苯基)-7-(4-羟基苯基)-5,6-二氢萘-2-醇的汇聚合成策略, 其合成过程简洁, 不存在区域选择性难题.
陈盼盼 , 冯晓伟 , 陆智彭 , 厉廷有 . 选择性雌激素受体降解剂(S)-8-(4-(1-(3-氟丙基)吡咯烷-3-基)氧基)苯基)-7-(4-羟基苯基)-5,6-二氢萘-2-醇的汇聚合成[J]. 有机化学, 2024 , 44(11) : 3550 -3555 . DOI: 10.6023/cjoc202403009
A more feasibly convergent synthesis of selective estrogen receptor degrading agent (S)-8-(4-((1-(3-fluoropropyl)- pyrrolidin-3-yl)oxy)phenyl)-7-(4-hydroxyphenyl)-5,6-dihydronaphthalen-2-ol was reported, featured with concise work up and absence of regioselectivity dilemma.
| [1] | Sung H.; Ferlay J.; Siegel R.; Laversanne M.; Soerjomataram I.; Jemal A.; Freddie Bray F. Ca-Cancer J. Clin. 2021, 71, 209. |
| [2] | Tang J.; Wu Z.; Tian Z.; Chen W.; Wu G. Cell Death Discovery 2021, 12, 534. |
| [3] | Huang B.; Omoto Y.; Iwase H.; Yamashita H.; Toyama T.; Coombes R.; Filipovic A.; Warner M.; Gustafsson J. Proc. Natl. Acad. Sci. U. S. A. 2014, 111, 1933. |
| [4] | Burstein H. N. Engl. J. Med. 2020, 383, 2557. |
| [5] | Jin M.; Yang L.; Jeong K. Theranostics 2022, 12, 5761. |
| [6] | Ma C.; Reinert T.; Chmielewska I.; Ellis M. Nat. Rev. Cancer 2015, 15, 261. |
| [7] | Osborne C.; Pippen J.; Jones S.; Parker L.; Ellis M.; Come S.; Gertler S.; May J.; Burton G.; Dimery I.; Webster A.; Morris C.; Elledge R.; Buzdar A. J. Clin. Oncol. 2002, 20, 3386. |
| [8] | Wakeling A.; Dukes M.; Bowler J. Cancer. Res 1991, 51, 3867. |
| [9] | Kruchten M.; de Vries E.; Glaudemans A.; van Lanschot M.; van Faassen M.; Kema I.; Brown M.; Schr?der C.; de Vries E.; Hospers G. Cancer Discovery 2015, 5, 72. |
| [10] | El-Ahmad Y.; Tabart M.; Halley F.; Certal V.; Thompson F.; Filoche-Rommé B.; Gruss-Leleu F.; Muller C.; Brollo M.; Fabien L.; Loyau V.; Bertin L.; Richepin P.; Pilorge F.; Desmazeau P.; Girardet C.; Beccari S.; Louboutin A.; Lebourg G.; Le-Roux J.; Terrier C.; Vallée F.; Steier V.; Mathieu M.; Rak A.; Abecassis P.; Vicat P.; Benard T.; Bouaboula M.; Sun F.; Shomali M.; Hebert A.; Levit M.; Cheng H.; Courjaud A.; Ginesty C.; Perrault C.; Garcia-Echeverria C.; McCort G.; Schio L. J. Med. Chem. 2020, 63, 512. |
/
| 〈 |
|
〉 |
