CAS: 128607-22-7; 2-[4-[(Z)-4-Chloro-1,2-Diphenylbut-1-Enyl]Phenoxy]Ethanol

该化合物是一种选择性雌激素受体受体调节器(SERM),主要用于治疗阴道疏松症,其特点是与更年期有关的阴道萎缩导致痛苦性交,其特点是与更年期有关的阴道萎缩.作为一种非类化合物,它表现出组织选择性的雌激素诱变活动,意味着它在某些组织中可以模仿雌激素,同时阻止其在其他组织中的影响.Ospemifene因其通过提高阴道组织厚度和弹性促进阴道和体外健康的能力而著称,从而缓解不适.该物质的生物利用率相对较低,在肝脏中被新陈代谢,其致癌作用受到各种因素的影响,包括年龄和肝功能.常见的副作用可能包括热闪光,阴道排出以及与雌激素疗法有关的潜在风险,如血栓栓血栓博事件.Ospememifene的独特行动机制及其有针对性的方法使得它成为管理出室症状的重要选择,特别是在那些不能或不愿使用传统激素疗法的妇女中.

结构式图片

欧盟法规

ECHA物质C&L通报

上下游产品

CAS号936-59-4 3-氯代苯丙酮 | CAS号14814-17-6 (4-(2-羟基乙氧基)苯基)... | CAS号177989-80-9 (Z)-(1-(4-(2-(b... | CAS号89778-41-6 Phenol, 4-[(1Z)... | CAS号96388-83-9 四氢-2-(2-碘乙氧基)-2H-吡喃 | CAS号341527-08-0 (Z)-[4-(4-Chlor... | CAS号58214-99-6 2-phenoxyethyl ... | CAS号65-85-0 苯甲酸 | CAS号122-99-6 乙二醇苯醚

合成工艺路线路线简述

    (Z)-(1-(4-(2-(Benzyloxy)Ethoxy)Phenyl)-4-Chlorobut-1-Ene-1,2-Diyl)Dibenzene置于钯 氢气,钯,乙醇,水体系中,用 乙酸乙酯,乙醇 用作溶剂,化学反应生成欧司哌米
    参考文献:Triphenylethylenes For The Prevention And Treatment Of Osteoporosis
    标题:Triphenylethylenes For The Prevention And Treatment Of Osteoporosis
    摘要:具有公式(i)的化合物,其中r.Sub.1和r.Sub.2独立地为h或oh,对于骨质疏松症的治疗和预防是有用的.公式(i)的化合物不具有明显的抗雌激素和雌激素活性.##str1##

    海关参考信息

    专利信息


    专利号:US-11873305-B2
    优先权日:2020-06-30
    标题 :Processes for synthesis of substituted indole intermediates for the synthesis of serd compounds
    发明人:ZHANG HAIMING; XU JIE; WUITSCHIK GEORG; ANGELAUD REMY; HEROLD SEBASTIAN; STUTZ ALFRED; BRUETSCH TOBIAS; BURKHARD JOHANNES
    权利人:GENENTECH INC; HOFFMANN LA ROCHE
    摘要:Provided herein are processes for the preparation of indolyl intermediates using Wenker Synthesis for the total synthesis of SERD compounds useful in the treatment of cancer.

    专利号:US-12043612-B2
    优先权日:2020-05-09
    标 题 :Methods of manufacturing a bifunctional compound, ultrapure forms of the bifunctional compound, and dosage forms comprising the same
    发明人:ALLAN LAURA E N; CHEN CHUNGPIN HERMAN; DONG HANQING; GROSSO JOHN A; HASKELL III ROYAL J; LLOYD RHYS; REECE HAYLEY
    权利人:ARVINAS OPERATIONS INC
    摘要:The present disclosure relates to ultra-pure forms, polymorphs, amorphous forms, and formulations of N-[(1r,4r)-4-(3-chloro-4-cyanophenoxy)cyclohexyl]-6-[4-({4-[2-(2,6-dioxopiperidin-3-yl)-6-fluoro-1,3-dioxo-2,3-dihydro-1H-isoindol-5-yl]piperazin-1-yl}methyl)piperidin-1-yl]pyridazine-3-carboxamide, referred to herein as Compound A:The present disclosure also relates methods of manufacturing and purifying the same, as well as intermediates useful in the synthesis of Compound A. The ultra-pure forms, polymorphs, amorphous forms, and formulations of Compound A can be used as therapeutic agents for the treatment of various diseases and conditions such as cancer.

    专利号:US-9975832-B2
    优先权日:2014-12-29
    标题:Process for the preparation of ospemifene and fispemifene
    发明人:CRISTIANO TANIA; ALPEGIANI MARCO
    权利人:OLON SPA
    摘要:Disclosed is a process for the synthesis of the active ingredients ospemifene and fispemifene which comprises reacting phenol 4 with an alkylating agent X—CH 2 CH 2 —Y of formula 7, wherein X is a leaving group and Y is the —(OCH 2 CH 2 ) n OH group wherein n is zero or 1; or X and Y, taken together, represent an oxygen atom; to give ospemifene or fispemifene of formula 8.

    专利号:US-2024174678-A1
    优先权日:2020-06-30
    标 题 :Processes for synthesis of substituted indole intermediates for the synthesis of serd compounds

    专利号:US-11780834-B2
    优先权日:2018-06-21
    标题:Solid forms of 3-((1R,3R)-1-(2,6-difluoro-4-((1-(3-fluoropropyl)azetidin-3- yl)amino)phenyl)-3-methyl-1,3,4,9-tetrahydro-2H-pyrido[3,4-b]indol-2-yl)-2,2-difluoropropan-1-ol and processes for preparing fused tricyclic compounds comprising a substituted phenyl or pyridinyl moiety, including methods of their use
    发明人:CHUNG CHEOL KEUN; XU JIE; IDING HANS; CLAGG KYLE; DALZIEL MICHAEL; FETTES ALEC; GOSSELIN FRANCIS; LIM NGIAP-KIE; MCCLORY ANDREW; ZHANG HAIMING; CHAKRAVARTY PAROMA; NAGAPUDI KARTHIK; ROBINSON SARAH
    权利人:HOFFMANN LA ROCHE; GENENTECH INC
    摘要:Provided herein are solid forms, salts, and formulations of 3-((1R,3R)-1-(2,6-difluoro-4-((1-(3-fluoropropyl)azetidin-3-yl)amino)phenyl)-3-methyl-1,3,4,9-tetrahydro-2H-pyrido[3,4-b]indol-2-yl)-2,2-difluoropropan-1-ol, processes and synthesis thereof, and methods of their use in the treatment of cancer.

    专利号:JP-7273802-B2
    优先权日:2017-08-28
    标题 :Asymmetric Synthesis of Compounds and Use in Disease Treatment
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    主要参考文献


    1: Di Carlo C, Cagnacci A, Murina F, Maffei S, Becorpi A, Lello S. Ospemifene and vulvovaginal atrophy: an update of the clinical profile for post-menopausal women. Expert Opin Pharmacother. 2024 Aug 12. doi: 10.1080/14656566.2024.2391009. Epub ahead of print.
    16:1049-1053. doi: 10.2147/IJWH.S431520.
    3: Meriggiola MC, Villa P, Maffei S, Becorpi A, Di Paolantonio T, Nicolucci A, Salvatore S, Nappi RE; PEONY Study Group. Vulvovaginal atrophy in women with and without a history of breast cancer: Baseline data from the PatiEnt satisfactiON studY (PEONY) in Italy. Maturitas. 2024 May;183:107950. doi: 10.1016/j.maturitas.2024.107950. Epub 2024 Mar 5. 66(1697):33-38. doi: 10.58347/tml.2024.1697a. 15(11):e49079. doi: 10.7759/cureus.49079.

    合成参考文献


    摘要:S109 | PARCEDC | List of 7074 potential endocrine disrupting compounds (EDCs) by PARC T4.2 | DOI:10.5281/zenodo.10944198
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