CAS: 110025-28-0; 4-(1-(4-(2-(Methylamino)Ethoxy)Phenyl)-2-Phenylbut-1-En-1-yl)Phenol

该化合物是三氧化锡的一种活性代谢物,一种选择性雌激素受体调节器(SERM),该复合物对药理研究具有重大兴趣,因为它在研究三氧化锡新陈代谢和雌激素受体相互作用方面的作用.E/Z异构体的大约1:1之比为调查立体化学对生物活动的影响提供了一种有代表性的混合物.其结构特征,包括四方的氢氧基化合物和N-甲基混合物的不存在,促成了与母体化合物相比受体结合的改变.这一产品主要用于分析和机械研究,以阐明四氧化物的代谢途径和治疗机制.

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上下游产品

CAS号74-89-5 氨基甲烷 | CAS号103-65-1 正丙苯溶液标准物质 | CAS号61002-54-8 4-Hydroxyphenyl... | CAS号115499-97-3 [4-(methoxymeth... | CAS号850256-19-8 E/Z-1-(4-hydrox... | CAS号671791-56-3 1-(4-methoxymet... | CAS号850256-21-2 E/Z-1-[4-(2-bro...

合成工艺路线路线简述

  • 合成目标产物 N-Desmethyl-4-Hydroxy Tamoxifen (Approx. 1:1 E/z Mixture) 主要起始原料 4,4'-Dihydroxybenzophenone
  • (文献来源)合成步骤主要原料 4,4'-Dihydroxybenzophenone

海关参考信息

专利信息


专利号:WO-2017080770-A1
优先权日:2015-11-10
标题 :Synthesis of (z)-endoxifen hydrochloride
发明人：HEINKELE GEORG; MUERDTER THOMAS; SCHWAB MATTHIAS
权利人:ROBERT BOSCH GES FÃœR MEDIZINISCHE FORSCHUNG MBH
摘要:The invention relates to the synthesis of tamoxifen, endoxifen and derivatives thereof. Starting from a substituted benzoic acid derivative and 2-phenoxyethyl halide, the intermediate product of general formula (I) is obtained. The compound of general formula (VI) or a salt thereof is obtained from the compound of general formula (I), via isomer purification of the compound of general formula (I) by obtaining the (Z)-isomers and reacting the (Z)-isomers with an amine of formula HNR 6 R 7 . Alternatively, the compound of general formula (I) is reacted with a compound of formula HNR 6 R 7 , and the amine thus obtained is then subjected to isomer purification, wherein the compound of general formula (VI) or a salt thereof is obtained.

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.

专利号:US-2025241876-A1
优先权日:2023-07-19
标 题:Anti-tumor compounds and methods of use thereof and synthesis thereof
发明人：QUAY STEVEN CARL
权利人:ATOSSA THERAPEUTICS INC
摘要:Described herein are pharmaceutical compounds and compositions and methods of making thereof. Methods of synthesis for the compounds are described herein. The compounds or compositions described herein may exhibit aromatase inhibition activity or estrogen receptor activity. The compounds and compositions described herein may be useful in the treatment of a condition in a subject.

专利号:DE-102015222031-A1
优先权日:2015-11-10
标题 :Synthesis of (Z) -endoxifene hydrochloride

专利号:WO-2025019830-A1
优先权日:2023-07-19
标 题:Anti-tumor compounds and methods of use thereof and synthesis thereof

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合成参考文献


参考文献:10.1200/jco.2010.32.9839
摘要:de Graan AJ, Teunissen SF, de Vos FY, Loos WJ, van Schaik RH, de Jongh FE, de Vos AI, van Alphen RJ, van der Holt B, Verweij J, Seynaeve C, Beijnen JH, Mathijssen RH. Dextromethorphan as a phenotyping test to predict endoxifen exposure in patients on tamoxifen treatment. J Clin Oncol. 2011 Aug 20;29(24):3240–6. doi: 10.1200/jco.2010.32.9839.
参考文献:10.1200/jco.2011.36.3895
摘要:Rae JM. Personalized tamoxifen: what is the best way forward J Clin Oncol. 2011 Aug 20;29(24):3206–8. doi: 10.1200/jco.2011.36.3895.
参考文献:10.1200/jco.2010.31.4427
摘要:Irvin WJ, Walko CM, Weck KE, Ibrahim JG, Chiu WK, Dees EC, Moore SG, Olajide OA, Graham ML, Canale ST, Raab RE, Corso SW, Peppercorn JM, Anderson SM, Friedman KJ, Ogburn ET, Desta Z, Flockhart DA, McLeod HL, Evans JP, Carey LA. Genotype-guided tamoxifen dosing increases active metabolite exposure in women with reduced CYP2D6 metabolism: a multicenter study. J Clin Oncol. 2011 Aug 20;29(24):3232–9.
参考文献:10.1016/j.ejmech.2011.07.005
摘要:Bourassa P, Dubeau S, Maharvi GM, Fauq AH, Thomas TJ, Tajmir-Riahi HA. Locating the binding sites of anticancer tamoxifen and its metabolites 4-hydroxytamoxifen and endoxifen on bovine serum albumin. European Journal of Medicinal Chemistry. 2011 Sep;46(9):4344–53. doi: 10.1016/j.ejmech.2011.07.005.
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