CAS: 1032008-74-4; (Z)-4-(1-(4-(2-(Methylamino)Ethoxy)Phenyl)-2-Phenylbut-1-En-1-yl)Phenol Hydrochloride
- 英文名称(Z)-4-(1-(4-(2-(Methylamino)Ethoxy)Phenyl)-2-Phenylbut-1-En-1-yl)Phenol Hydrochloride
- 中文名称Z-因多昔芬盐酸盐
- IUPAC名称(Z)-4-(1-(4-(2-(methylamino)ethoxy)phenyl)-2-phenylbut-1-en-1-yl)phenol hydrochloride
- CAS编号1032008-74-4
- MFCD编号:MFCD29049515
- FDA UNII编号:308PA1L567
- 分子式:C25H28ClNO2分子量:409.95
- 产品CID: 65774
- 同类组份化合物CAS1032008-74-4 (HCl)112093-28-4 (free base)1372937-28-4 (citrate)1032008-66-4 (acetate)1032008-71-1 (mesylate)1197194-61-8 (E-isomer HCl)
- 产品分类生物化工 → 生化试剂 → 激动剂抑制剂
MSDS等安全信息
合成工艺路线路线简述
📜(4-Hydroxyphenyl)(4-(2-(Methylamino)Ethoxy)Phenyl)Methanone Hydrochloride,苯丙酮置于四氯化钛,锌体系中,用 四氢呋喃 用作溶剂,化学反应生成(E)-4-羟基-N-去甲基他莫昔芬,Z-因多昔芬盐酸盐
参考文献:A Convenient Synthesis Of (Z)-4-Hydroxy-N-Desmethyltamoxifen (Endoxifen)
标题:A Convenient Synthesis Of (Z)-4-Hydroxy-N-Desmethyltamoxifen (Endoxifen)
摘要:A Mixture Of The (Z)-And (E)-Isomers Of 4-Hydroxy-N-Desmethyltamoxifen Was Conveniently Prepared In Four Steps. These Geometrical Isomers Were Then Neatly Separated By Semi-Preparative Reverse Phase High Performance Liquid Chromatography (Rp-HPLC) Using Specified Conditions. Additionally,The Isolated E-Isomer Could Be Equilibrated In Aqueous Strong Acid In Acetonitrile Or Trifluoroacetic Acid/dichloromethane To Give A Clean 1: 1 Mixture Of Z/e Isomers That Was Re-Subjected To HPLC Separation. In This Way,Most Of The Undesired (E)-Isomer Could Be Readily Converted To The Desired (Z)-Isomer Providing Quick Access To Over 200 Mg Quantities Of Pure Endoxifen (Z-Isomer),A Potent Antiestrogenic Metabolite Of Tamoxifen Traditionally Used In Breast Cancer Treatment. (C) 2010 Elsevier Ltd. All Rights Reserved.
Doi:10.1016/j.Bmcl.2010.03.117
海关参考信息
- 2905199090-其他饱和一元醇
2905399099-其他二元醇
2905499000-其他多元醇
2905590090-其他无环醇的卤化、磺化等衍生物 - 💡 提示：海关信息按照顺序优先匹配，如需确认的海关信息，请参考相关资料。
- 详情请参考：📖 海关编码查询和海关进出口税则
专利信息
专利号:WO-2025019775-A1
优先权日:2023-07-19
标题 :Endoxifen compositions and methods of use thereof and synthesis thereof
发明人：QUAY STEVEN
权利人:ATOSSA THERAPEUTICS INC
摘要:Described herein are endoxifen compositions comprising novel compounds and methods of use thereof. Methods of synthesis for the compositions are described herein. The endoxifen compositions described herein may exhibit aromatase inhibition activity or estrogen receptor activity. The endoxifen compositions described herein may be useful in the treatment of a condition in a subject, such as cancer.
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主要参考文献
1. Chao TC, Pan WC, Tsai YF, Chou YC, Liu YR, Wang SF, Chen YJ, Souček P, Ueng YF. Plasma endoxifen and 4-hydroxytamoxifen levels in CYP2D6(C100T) carrying breast cancer patients and association with serum cholesterol. Toxicol Appl Pharmacol. 2019 Sep 1;378:114619. doi: 10.1016/j.taap.2019.114619. Epub 2019 Jun 10. Erratum in: Toxicol Appl Pharmacol. 2019 Oct 1;380:114701. doi: 10.1016/j.breast.2019.05.009. Epub 2019 May 6. doi: 10.1080/17512433.2019.1610390. Epub 2019 Apr 30. Review. No abstract available. doi: 10.1124/mol.117.111385. Epub 2018 May 8. doi: 10.1016/j.bmcl.2018.03.008. Epub 2018 Mar 13. doi: 10.1186/s11658-017-0068-7. eCollection 2018. doi: 10.1210/en.2016-1871. doi: 10.3389/fphar.2017.00582. eCollection 2017. doi: 10.1200/JCO.2017.73.3246. Epub 2017 Aug 30. doi: 10.1200/JCO.2017.74.9325. Epub 2017 Aug 30. No abstract available. doi: 10.2174/1872312811666170815160751. doi: 10.1038/tpj.2017.36. Epub 2017 Aug 1. Review. doi: 10.1007/s40262-017-0555-z. doi: 10.1007/s00726-016-2300-6. Epub 2016 Jul 20. doi: 10.1111/cts.12407. Epub 2016 Jun 27. Erratum in: Clin Transl Sci. 2017 Mar;10 (2):117. doi: 10.1158/1078-0432.CCR-15-1470. Epub 2016 Feb 4. doi: 10.1007/s10549-015-3562-5. Epub 2015 Sep 14. doi: 10.1007/s10549-015-3461-9. Epub 2015 Jun 14. doi: 10.1016/j.ejphar.2015.01.048. Epub 2015 Feb 11. [citation] PMID: 25680947
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