CAS: 569-57-3; 4,4',4''-(2-Chloroethene-1,1,2-Triyl)Tris(Methoxybenzene)

该化合物是合成非类静态雌激素化合物,主要用于激素疗法和研究应用;其化学结构由三种甲氧基组组成,有助于其雌激素活动和代谢稳定性;该化合物历来用于治疗更年期症状和某些激素不平衡,因为其具有模仿内生雌激素效应的能力;氯硝基苯因其代谢解裂和组织积累缓慢,行动时间长.尽管其临床用途随着新制剂的出现而下降,但在研究雌激素受体相互作用和激素途径的生物化学研究中仍然具有相关性.

结构式图片

上下游产品

CAS号100-66-3 苯甲醚 | CAS号61161-13-5 1,2,2-tris(4-me... | CAS号1076-95-5 2-(4-甲氧基苯基)-2-氧代乙醛 | CAS号25354-46-5 1-bromo-1,2,2-t... | CAS号72-43-5 甲氧滴滴涕 | CAS号17105-65-6 DIMETHYL(4-METH... | CAS号824-94-2 4-甲氧基苄氯 | CAS号90-96-0 4,4'-二甲氧基二苯甲酮 | CAS号86457-76-3 Dimethyl 1-chlo... | CAS号14062-18-1 对甲氧基苯乙酸乙酯 | CAS号1040086-21-2 9-chloro-3,6-di... | CAS号90-96-0 4,4'-二甲氧基二苯甲酮 | CAS号7109-27-5 Benzene,1,1',1'...

合成工艺路线路线简述

    📜苯甲醚置于五氯化磷,硫酸,溶剂黄146,甲苯体系中,化学反应生成 氯烯雌醚
    参考文献:Preparations Of The Synthetic Estrogens. Vii.1 New Syntheses Of 1,1,2-Tri-P-Anisyl-2-Chloroethylene
    标题:Preparations Of The Synthetic Estrogens. Vii.1 New Syntheses Of 1,1,2-Tri-P-Anisyl-2-Chloroethylene
    摘要:
    DOI:10.1021/ja01629A046

    海关参考信息

    专利信息


    专利号:US-2004006137-A1
    优先权日:2002-06-28
    标题:Asymmetric synthesis of amino-pyrrolidinones and a crystalline, free-base amino-pyrrolidinone
    发明人:WALTERMIRE ROBERT E; CAMPAGNA SILVIO; SAVAGE SCOTT A; BORDAWEKAR SHAILENDRA; MADUSKUIE THOMAS P; DESIKAN SRIDHAR; ANDERSON STEPHEN R
    摘要:A novel process for the asymmetric synthesis of an amino-pyrrolidinone of the type shown below is described. n n n These compounds are useful as intermediates for MMP and TACE inhibitors. n Crystalline, free-base form of Compound J ((2R)-2-((3R)-3-amino-3-{-[(2-methyl-4-quinolinyl)methoxy]phenyl}-2-oxopyrrolidinyl)-N-hydroxy-4-methylpentanamide): n n n which is useful as a TACE inhibitor, pharmaceutical compositions comprising the same, and methods of using the same for treating inflammatory diseases are also described.

    专利号:US-2004033532-A1
    优先权日:2002-08-08
    标题 :Use of three-dimensional crystal structure coordinates to design and synthesize domain-selective inhibitors for angiotensin-converting enzyme (ACE)
    发明人:EHLERS MARIO R W; HOLMQUIST BARTON
    摘要:It has now been discovered that the use of the three-dimensional crystal structure coordinates of angiotensin-converting enzyme (ACE) will enable the design and synthesis, by means of computational chemistry and structure-guided drug design, of inhibitors of ACE that are highly selective and specific for either the N domain or the C domain of the enzyme, for the treatment of diverse diseases. The invention also relates to methods and processes for the structure-guided design and synthesis of dual N- and C-domain ACE inhibitors, and inhibitors that operate by competitive, non-competitive, uncompetitive, and irreversible mechanisms.

    专利号:US-6906046-B2
    优先权日:2000-12-22
    标题 :Pharmaceutical uses and synthesis of benzobicyclooctanes
    发明人:JACKSON RANDY W; DARWISH IHAB; BAUGHMAN TED A; HOWBERT J JEFFRY
    权利人:CELLTECH R & D INC
    摘要:Benzobicyclooctane compounds, their use in inhibiting cellular events involving TNF-α and IL-8, and in the treatment of inflammation events in general; a combinatorial library of diverse bicyclooctanes and process for their synthesis as a library and as individual compounds.

    专利号:US-2003157061-A1
    优先权日:2001-12-05
    标 题 :Combinations of a cyclooxygenase-2 selective inhibitor and a TNFalpha antagonist and therapeutic uses therefor
    发明人:BENNETT DENNIS A
    权利人:PHARMACIA CORP
    摘要:A method for the prevention, treatment, or inhibition of pain, inflammation, or inflammation-related disorder and for the prevention, treatment, or inhibition of a cardiovascular disease or disorder in a subject that is in need of such prevention, treatment or inhibition, involves the administration to the subject of a cyclooxygenase-2 selective inhibitor or prodrug thereof and a TNFα antagonist. A method can also involve the treatment, prevention, or inhibition of cancer in a subject in need of such treatment, prevention, or inhibition, by administering to the subject a cyclooxygenase-2 selective inhibitor or prodrug thereof and a TNFα antagonist which is selected from the group consisting of a compound that affects the synthesis of TNFα, a compound that inhibits the binding of TNFα with a receptor specific for TNFα, and a compound that interferes with intracellular signaling triggered by TNFα binding with a receptor. Compositions, pharmaceutical compositions and kits that can be used with the methods are also described.

    专利号:US-8710261-B2
    优先权日:2005-02-22
    标 题:5-phenyl-pentanoic acid derivatives as matrix metalloproteinase inhibitors for the treatment of asthma and other diseases
    发明人:PALLE VENKATA P; SATTIGERI VISWAJANANI JITENDRA; KHERA MANOJ KUMAR; VOLETI SREEDHARA RAO; RAY ABHIJIT; DASTIDAR SUNANDA G
    权利人:PALLE VENKATA P; SATTIGERI VISWAJANANI JITENDRA; KHERA MANOJ KUMAR; VOLETI SREEDHARA RAO; RAY ABHIJIT; DASTIDAR SUNANDA G; RANBAXY LAB LTD
    摘要:The present invention relates to Compounds having the structure of Formula I: wherein n is an integer from 1 to 5; R 1 is optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heterocyclyl, heteroaryl, aralkyl, alkoxy, aryloxy, alkenyloxy or alkynyloxy; R 2 is alkenyl, allcynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, NR 4 R 5 , —NHC(â•?Y)R 4 , —NHC(â•?Y)NR 5 R χ , —NHC(â•?O)OR 4 , —NHSO 2 R 4 , C(â•?Y)NR 4 R 5 , C(â•?O)OR 6 [wherein Y is oxygen or sulphur], OR 5 , —O(Câ•?O)NR 4 R 5 , O-acyl, S(O) m R 4 , —SO 2 N(R 4 ) 2 , cyano, amidino or guanidino [wherein R 4 is alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heterocyclyl, heteroaryl, aralkyl, heteroarylalkyl, heterocyclylalkyl or cycloalkylalkyl and m is an integer 0-2; R 5 is hydrogen or R 4 ; R x is R 4 or —SO 2 N(R 4 ) 2 and R 6 is hydrogen, alkyl, cycloalkyl, aralkyl, heteroarylalkyl, heterocyclylalkyl or cycloalkylalkyl]; R 3 is hydrogen, fluorine, alkyl, cycloalkylalkyl or aralkyl; A is OH, OR 4 , —OC(â•?O)NR 4 R 5 , O-acyl, NH 2 , NR 4 R 5 , —NHC(â•?Y)R 4 , —NHC(â•?Y)NR 5 R x , —NHC(â•?O)OR 4 , —NHSO 2 R 4 , and to processes for the synthesis of the same. This invention also relates to pharmacological compositions containing the compounds of the present invention, and methods of treating asthma, rheumatoid arthritis, COPD, rhinitis, osteoarthritis, psoriatic arthritis, psoriasis, pulmonary fibrosis pulmonary inflammation, acute respiratory distress syndrome, perodontitis, multiple sclerosis, gingivitis, atherosclerosis, neointimal proliferation, which leads to restenosis and ischemic heart failure, stroke, renal diseases, tumor metastasis, and other inflammatory disorders characterize by over-expression and over-activation of an matrix metalloproteinase, using the compounds.

    专利号:US-7288671-B2
    优先权日:1999-05-14
    标题:Interleukin-1 and tumor necrosis factor-α modulators, synthesis of said modulators and their enantiomers and methods of using said modulators
    发明人:PALLADINO MICHAEL; THEODORAKIS EMMANUEL A
    权利人:UNIV CALIFORNIA
    摘要:Novel compounds are disclosed that have the following chemical structures, and prodrug esters and acid-addition salts thereof, that are useful as Interleukin-1 and Tumor Necrosis Factor-α modulators, and thus are useful in the treatment of various diseases. n nwherein the R groups are defined as follows: if any R 3 -R 5 , R 7 , R 8 , R 11 -R 13 is not hydrogen, R 2 or R 6 or R 9 is not methyl, or R 10 is not CH 2 , then R 1 is selected from the group consisting of hydrogen, a halogen, COOH, C 1 -C 12 carboxylic acids, C 1 -C 12 acyl halides, C 1 -C 12 acyl residues, C 1 -C 12 esters, C 1 -C 12 secondary amides, (C 1 -C 12 )(C 1 -C 12 ) tertiary amides, (C 1 -C 12 )(C 1 -C 12 ) cyclic amides, (C 1 -C 12 ) amines, C 1 -C 12 alcohols, (C 1 -C 12 )(C 1 -C 12 ) ethers, C 1 -C 12 alkyls, C 1 -C 12 substituted alkyls, C 2 -C 12 alkenyls, C 2 -C 12 substituted alkenyls, and C 5 -C 12 aryls. If all R 3 -R 5 , R 7 , R 8 , R 11 -R 13 are hydrogen, R 2 , R 6 , and R 9 are each methyl, and R 10 is CH 2 , then R 1 is selected from hydrogen, a halogen, C 1 -C 12 carboxylic acids, C 1 -C 12 acyl halides, C 1 -C 12 acyl residues, C 2 -C 12 esters, C 2 -C 12 secondary amides, (C 1 -C 12 )(C 1 -C 12 ) tertiary amides, C 2 -C 12 alcohols, (C 1 -C 12 )(C 1 -C 12 ) ethers other than methyl-acetyl ether, C 2 -C 12 alkyls, C 1 -C 12 substituted alkyls, C 2 -C 12 alkenyls, C 2 -C 12 substituted alkenyls, and C 2 -C 12 aryls. R 2 and R 9 are each separately selected from hydrogen, a halogen, C 1 -C 12 alkyl, C 1 -C 12 substituted alkyls, C 2 -C 12 alkenyl, C 2 -C 12 substituted alkenyl, C 2 -C 12 alkynyl, C 1 -C 12 acyl, C 1 -C 12 alcohol, and C 5 -C 12 aryl. R 3 -R 5 , R 7 , R 8 , and R 11 -R 13 are each separately selected from hydrogen, a halogen, C 1 -C 12 alkyl, C 1 -C 12 substituted alkyls, C 2 -C 12 alkenyl, C 2 -C 12 substituted alkenyl, C 2 -C 12 alkynyl, and C 5 -C 12 aryl. R 6 is selected from hydrogen, a halogen, C 1 -C 12 alkyl, C 1 -C 12 substituted alkyls, C 2 -C 12 alkenyl, C 2 -C 12 substituted alkenyl, and C 2 -C 12 alkynyl. R 10 is selected from hydrogen, a halogen, CH 2 , C 1 -C 6 alkyl, C 1 -C 6 substituted alkyl, C 2 -C 6 alkenyl, C 2 -C 6 substituted alkenyl, C 1 -C 12 alcohol, and C 5 -C 12 aryl. Pharmaceutical compositions comprising, and uses of, therapeutically effective amounts of the aove compounds and their prodrug esters, and a pharmaceutically acceptable carrier, are also disclosed, and are useful as, for example, anti-inflammatory analgesics, in treating immune disorders, as anti-cancer and anti-tumor agents, and in the treatment of cardiovascular disease, skin redness, and viral infection. Completely synthetic and semi-synthetic methods of making these compounds and their analogs, are also disclosed.

    供应商参考报价(招募中)

    品牌试剂参考报价(招募中)

    📌 第三方产品分析报告

    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Zhang J, Yang W, Shen Z. [Prevention of bone loss by chlorotrianisene in oophorectomized rats]. Zhonghua Fu Chan Ke Za Zhi. 1997 Sep;32(9):535-7. Chinese. French. French. Russian. German. Italian. Italian. French. French. Presse Med. 1955 Sep 14;63(59):1198. French.

    合成参考文献


    摘要:Osol, A. and J.E. Hoover, et al. (eds.). Remington's Pharmaceutical Sciences. 15th ed. Easton, Pennsylvania: Mack Publishing Co., 1975., p. 918
    摘要:The Merck Index. 9th ed. Rahway, New Jersey: Merck & Co., Inc., 1976., p. 271
    摘要:S109 | PARCEDC | List of 7074 potential endocrine disrupting compounds (EDCs) by PARC T4.2 | DOI:10.5281/zenodo.10944198
    参考文献:10.1007/s11934-004-0036-4
    摘要:Miyamoto H, Messing EM. Early versus late hormonal therapy for prostate cancer. Curr Urol Rep. 2004 Jun;5(3):188–96. doi: 10.1007/s11934-004-0036-4.
    参考文献:10.1111/j.1600-0773.1966.tb00371.x
    摘要:Terenius L. Effect of synthetic oestrogens and analogues on the uptake of oestradiol by the immature mouse uterus and vagina. Acta Pharmacol Toxicol (Copenh). 1966;24(1):89–100. doi: 10.1111/j.1600-0773.1966.tb00371.x.
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