CAS: 116057-75-1; (E)-1-(2-(4-(1-(4-Iodophenyl)-2-Phenylbut-1-En-1-yl)Phenoxy)Ethyl)Pyrrolidine

该化合物是一种合成化合物,被归类为选择性雌激素受体调节器(SERM),主要研究该合成化合物在治疗乳腺癌和骨质疏松症方面的潜在用途,因为它能够有选择地与雌激素受体结合,模仿或阻塞不同组织中的雌激素影响.

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CAS号123-75-1 四氢吡咯 | CAS号116057-73-9 (E)-1-[4-(2-chl... | CAS号624-38-4 1,4-二碘苯 | CAS号103628-22-4 1-[4-(2-氯乙氧基)苯基... | CAS号370563-63-6 1-[4-(2-chloroe... | CAS号93-55-0 苯丙酮 | CAS号122-99-6 乙二醇苯醚 | CAS号622-86-6 2-氯苯乙醚

合成工艺路线路线简述

    📜1-[4-(2-氯乙氧基)苯基]-2-乙基-2-苯乙酮置于盐酸,正丁基锂体系中,用 乙醇 用作溶剂,化学反应 26.17H,反应生成艾多昔芬
    参考文献:他莫昔芬的衍生物.抗雌激素性对4-取代基的依赖性.
    标题:他莫昔芬的衍生物.抗雌激素性对4-取代基的依赖性.
    摘要:描述了在1-苯环的4-位上取代的他莫昔芬衍生物的范围.合成4-碘-,4-溴-和4-(甲硫基)他莫昔芬的关键步骤是1,2-二芳基丁酮与(4-卤代苯基)锂或[4-(甲硫基)苯基]镁的反应溴化物.使用4-(甲硫基)他莫昔芬的氧化前体制备甲基亚磺酰基和甲基磺酰基衍生物.由4-溴苯莫西芬经由4-硫代衍生物制备其他衍生物(甲酰基,羟甲基,环氧乙烷,巯基).几种衍生物(br,I,Sme,Some,So2Me,环氧乙烷,Cho,Ch2Oh)对小牛子宫细胞溶质的雌激素受体(er)的亲和力高于他莫昔芬,但对er的亲和力与体外抑制mcf-7乳腺癌细胞系生长的能力.
    Doi:10.1021/jm00132A006

    海关参考信息

    专利信息


    专利号:US-12383499-B2
    优先权日:2018-01-01
    标题:Scale up synthesis of silicasome nanocarriers
    发明人:NEL ANDRE E; MENG HUAN; LIU XIANGSHENG
    权利人:UNIV CALIFORNIA
    摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).

    专利号:US-8734846-B2
    优先权日:2008-06-16
    标 题 :Methods for the preparation of targeting agent functionalized diblock copolymers for use in fabrication of therapeutic targeted nanoparticles
    发明人:ALI MIR M; HRKACH JEFF; ZALE STEPHEN E; ALVAREZ DE CIENFUEGOS LUIS
    权利人:BIND BIOSCIENCES INC
    摘要:This application provides nanoparticles and methods of making nanoparticles using pre-functionalized poly(ethylene glycol)(also referred to as PEG) as a macroinitiator for the synthesis of diblock copolymers. Ring opening polymerization yields the desired poly(ester)-poly (ethylene glycol)-targeting agent polymer that is used to impart targeting capability to therapeutic nanoparticles. This “polymerization fromâ€? approach typically employs precursors of the targeting agent wherein the reactivity of functional groups of the targeting agent is masked using protecting groups. Also described is a “coupling toâ€? that utilized the poly(ethylene glycol)-targeting agent conjugate where the targeting agent remains in its native un-protected form. This method uses “orthogonalâ€? chemistry that exhibit no cross reactivity towards functional groups typically found within targeting agents of interest.

    专利号:US-2013035307-A1
    优先权日:2010-01-26
    标 题:Methods for treating or preventing the spread of cancer using semi-synthetic glycosaminoglycosan ethers
    发明人:PRESTWICH GLENN D; KENNEDY THOMAS P
    权利人:UNIV UTAH RES FOUND; PRESTWICH GLENN D; KENNEDY THOMAS P
    摘要:Described herein are methods for the treatment and prevention of tumor metastasis using alkylated and fluoroalkylated semi-synthetic glycosaminoglycan ethers (“SAGEsâ€?). The synthesis of sulfated alkylated and fluoroalkylated SAGEs is also described.

    专利号:US-2008214827-A1
    优先权日:2004-02-03
    标 题:Synthesis of Cyanoimino-Benzoimidazoles
    发明人:GOEHRING R RICHARD; WHITEHEAD JOHN; SHAO BIN
    权利人:EURO CELTIQUE SA
    摘要:Disclosed in certain embodiments is a process for synthesizing a compound of formula (V) and salts thereof.

    专利号:US-2025289827-A1
    优先权日:2022-12-02
    标 题:Morphic forms of a mutant braf degrader and methods of manufacture thereof
    发明人:YU ROBERT T; HE MINSHENG; SCHNADERBECK MATTHEW J; KREGER BRIDGET; POLLOCK ROY MACFARLANE; JIANG SIYI; LI MEIQI; CHEN BOLU; LU JIANNAN
    权利人:C4 THERAPEUTICS INC
    摘要:Advantageous isolated morphic forms of (3R)-3-[6-[2-cyano-3-[[ethyl(methyl)sulfamoyl]amino]-6-fluorophenoxy]-4-oxoquinazolin-3-yl]-8-[2-[1-[3-(2,4-dioxo-1,3-diazinan-1-yl)-5-fluoro-1-methylindazol-6-yl]-4-hydroxypiperidin-4-yl]acetyl]-1-oxa-8-azaspiro[4.5]decane (Compound 1), which is a mutant BRAF degrader, and methods to prepare Compound 1 morphic forms for therapeutic applications are provided in the invention. The invention also provides improved methods for the synthesis of Compound 1, new pharmaceutical compositions comprising Compound 1, and new uses of Compound 1.

    专利号:US-9220714-B2
    优先权日:2006-03-16
    标 题 :Nitrofuran compounds for the treatment of cancer and angiogenesis
    发明人:SAULNIER SHOLLER GISELLE L; SWAMY NARASIMHA; KALKUNTE STAYAN; SINGH RAKESH K; BRARD LAURENT; KIM KYU KWANG
    权利人:WOMEN AND INFANTS HOSPITAL OF RHODE ISLAND; UNIV BROWN; WOMEN AND INFANTS HOSPITAL RHODE ISLAND
    摘要:The invention is directed to the synthesis and use of nitrofuran compounds, especially Nifurtimox, as medicaments to treat cancer, especially neuroblastoma, and to inhibit angiogenesis. The invention also provides compositions, unit dosage forms, and kits comprising the compounds.

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    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Rehm S, Solleveld HA, Portelli ST, Wier PJ. Histologic changes in ovary, uterus, vagina, and mammary gland of mature beagle dogs treated with the SERM idoxifene. Birth Defects Res B Dev Reprod Toxicol. 2007 Jun;80(3):225-32. Chinese. A cancer research (UK) randomized phase II study of idoxifene in patients with locally advanced/metastatic breast cancer resistant to tamoxifen. Cancer Chemother Pharmacol. 2004 Apr;53(4):341-8. Epub 2004 Jan 13.
    13: Omoya T, Shimizu I, Zhou Y, Okamura Y, Inoue H, Lu G, Itonaga M, Honda H, Nomura M, Ito S. Effects of idoxifene and estradiol on NF-kappaB activation in cultured rat hepatocytes undergoing oxidative stress. Liver. 2001 Jun;21(3):183-91.
    28: Johnston SR, Riddler S, Haynes BP, A'Hern R, Smith IE, Jarman M, Dowsett M. The novel anti-oestrogen idoxifene inhibits the growth of human MCF-7 breast cancer xenografts and reduces the frequency of acquired anti-oestrogen resistance. Br J Cancer. 1997;75(6):804-9.

    合成参考文献


    参考文献:10.7863/jum.1999.18.7.503
    摘要:Fleischer AC, Wheeler JE, Yeh IT, Kravitz B, Jensen C, MacDonald B. Sonographic assessment of the endometrium in osteopenic postmenopausal women treated with idoxifene. J Ultrasound Med. 1999 Jul;18(7):503–12. doi: 10.7863/jum.1999.18.7.503.
    参考文献:10.2165/00002512-199914050-00001
    摘要:Haynes B, Dowsett M. Clinical pharmacology of selective estrogen receptor modulators. Drugs Aging. 1999 May;14(5):323–36. doi: 10.2165/00002512-199914050-00001.
    参考文献:10.1007/bf02967993
    摘要:Garin AM. Breast cancer in Russia. Breast Cancer. 2004;11(1):7–9. doi: 10.1007/bf02967993.
    参考文献:10.1016/s0022-3565(24)35249-8
    摘要:Badger AM, Blake SM, Dodds RA, Griswold DE, Swift BA, Rieman DJ, Stroup GB, Hoffman SJ, Gowen M. Idoxifene, a Novel Selective Estrogen Receptor Modulator, Is Effective in a Rat Model of Adjuvant-Induced Arthritis. The Journal of Pharmacology and Experimental Therapeutics. 1999 Dec;291(3):1380–6. doi: 10.1016/s0022-3565(24)35249-8.
    参考文献:10.2165/00126839-199901030-00002
    摘要:Peters DC, Coleman SG. Osteoporosis. Summary and table. Drugs R D. 1999 Mar;1(3):203–9. doi: 10.2165/00126839-199901030-00002.
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