CAS: 15690-57-0; Trans-Clomiphene

该化合物是一种选择性雌激素受体调节器(SERM),主要用于治疗雄性低效和不孕症;它是三氯苯的立体异构体,在妇女生育治疗中常用;通过阻塞脊髓膜下腺的雌激素受体,导致蛋白激素的分泌增加,进而刺激雄性睾酮和精子的产生;这种复合体的特点是它能够选择性地调节雌激素活动,促进内生睾酮生产,同时尽量减少与传统睾酮替代疗法有关的副作用; 雌激素通常是口头施用,具有有利的药性肿瘤特征,允许体内的有效吸收和分布; 其治疗应用范围超出生殖力,因为它在与睾酮低水平有关的条件下也可能产生潜在好处; 但是,与任何药物一样,它必须考虑潜在的副作用和抗激素,其使用应以专业保健为指导.

结构式图片

MSDS等安全信息

    上下游产品

    (Z)-4-(2-Chloro-1,2-Diphenylethenyl) Methoxybenzene 72474-42-1
    Cis-1-Chloro-2-(4-Hydroxyphenyl)-1,2-Diphenylethylene 72474-40-9
    Deschloro Clomiphene

    合成工艺路线路线简述

      2-二乙氨基氯乙烷盐酸盐置于tris-(Dibenzylideneacetone)Dipalladium(0),Copper(L) Iodide,三苯胂,Sodium Ethanolate,Lithium Chloride,Copper Dichloride体系中,用 乙醇 用作溶剂,化学反应 130.0H,反应生成恩氯米芬
      参考文献:克罗米芬和他莫昔芬的立体有择合成二苯乙炔的锡铜
      标题:克罗米芬和他莫昔芬的立体有择合成二苯乙炔的锡铜
      摘要:摘要 二苯乙炔的立体有择反式-锡铜反应得到 1,2-二金属芪,通过钯催化与芳基碘偶联可将其加工成克罗米芬或他莫昔芬.
      Doi:10.1080/00397919508011484

      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-5817751-A
      优先权日:1994-06-23
      标 题 :Method for synthesis of diketopiperazine and diketomorpholine derivatives
      发明人:SZARDENINGS ANNA KATRIN; CAMPBELL DAVID
      权利人:AFFYMAX TECH NV
      摘要:The present invention relates to the areas of organic and medicinal chemistry. More specifically, the present invention is concerned with combinatorial and solid phase methods for the synthesis of diverse diketopiperazine derivatives, and the use of such methods to create libraries of diverse diketopiperazine derivatives. The present invention has application in the areas of chemical synthesis, the screening for new diketopiperazine derivatives having beneficial medical properties and the use of such screening to provide compositions and methods including diketopiperazine derivatives for treating disease.

      专利号:US-4895939-A
      优先权日:1986-02-24
      标题:High percentage β-yield synthesis of carbapenem intermediates
      发明人:MARTEL ALAIN; DARIS JEAN-PAUL; CORBEIL JACQUES
      权利人:BRISTOL MYERS CO
      摘要:Disclosed herein is a novel high beta -yield producing novel intermediates of the formula where R4 is useful in the synthesis of 1- beta -alkyl carbapenems.

      专利号:US-9902699-B2
      优先权日:2012-10-24
      标题 :Synthesis of tetrahydroisoquinolines from 2-methyl-1-phenyl substituted indenes
      发明人:ROSOCHA GREGORY; BATEY ROBERT
      权利人:ROSOCHA GREGORY; Gregory Rosocha
      摘要:A procedure for the synthesis of tetrahydroisoquinolines from 2-methyl-1-phenyl substituted indene is described. The process involves the use of osmium tetroxide to cleave the indene double bond forming the keto aldehyde product, which is then combined with a substituted amine forming the substituted isoquinoline. Isoquinolines can be useful as industrial products in the chemical, agrochemical, oil and gas industry, as well as useful as medicaments in the pharmaceutical industry.

      专利号:US-5633373-A
      优先权日:1989-07-07
      标 题 :Enantioselective synthesis of antifolates
      发明人:BARNETT CHARLES J; WILSON THOMAS M
      权利人:LILLY CO ELI
      摘要:A process and intermediates for the enantioselective synthesis of 5,10-dideaza-5,6,7,8-tetrahydrofolic acid are disclosed.

      专利号:US-5446203-A
      优先权日:1992-08-25
      标题:Synthesis of haloenones and aryl or alkyl substituted enones or alkenes
      发明人:MCNELIS EDWARD
      权利人:UNIV NEW YORK
      摘要:Alternative methods for synthesizing haloenones and haloakenes and their use as starting materials for synthesis of substituted or unsubstituted alkyl and aryl substituted enones and alkenes, including tamoxifen and tamoxifen analogs, using such haloenones and haloalkenes.
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      主要参考文献


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      合成参考文献


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      参考文献:10.1007/s00404-012-2672-0
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      摘要:Freis A, Renke T, Kämmerer U, Jauckus J, Strowitzki T, Germeyer A. Effects of a hyperandrogenaemic state on the proliferation and decidualization potential in human endometrial stromal cells. Archives of Gynecology and Obstetrics. 2017 Feb 06;295(4):1005–13. doi: 10.1007/s00404-017-4295-y.
      参考文献:10.1111/j.1439-0272.1992.tb02631.x
      摘要:Weissenberg R, Dar Y, Lunenfeld B. The effect of clomiphene citrate and its Zu or En isomers on the reproductive system of the immature male rat. Andrologia. 1992 May;24(3):161–5. doi: 10.1111/j.1439-0272.1992.tb02631.x.
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