CAS: 72-33-3; Mestranol

该化合物是一种合成雌激素,主要用于荷尔蒙避孕和激素替代疗法;一种白色的白白白脱白晶粉,在水中溶解不力,但在乙醇和氯仿等有机溶剂中溶解.Mestranol的特征是化学配方,包括一个苯丙基氢氧化物组,有助于其雌激素活动.物质对雌激素受体有约束力,影响各种生理过程,包括调节月经循环和保持第二性特征.Mestranol经常与口服避孕配方的预产物结合使用.其药理基因基因学涉及肝脏代谢,通常在尿液中分泌.虽然对预期用途有效,但甲基酚可以产生副作用,包括鼻涕,头痛和增加的血栓栓状事件风险.与任何激素治疗一样,医疗专业人员应仔细监测其使用情况,以减轻潜在风险和确保病人的安全.

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CAS号1624-62-0 雌酮-3-甲醚 | CAS号1066-54-2 三甲基硅基乙炔 | CAS号57-63-6 炔雌醇 | CAS号74-88-4 碘甲烷 | CAS号74-86-2 乙炔 | CAS号57-63-6 炔雌醇 | CAS号26011-40-5 2-羟基甲醇 | CAS号22415-44-7 2-Methoxy-Ethyn... | CAS号60134-76-1 乙炔雌二醇3-β-D-葡糖醛酸 | CAS号75803-39-3 乙炔雌二醇17-β-D-葡糖醛酸 | CAS号75812-41-8 17-ethynyl-1,2,... | CAS号1624-62-0 雌酮-3-甲醚 | CAS号10382-22-6 [(8R,9S,13S,14S... | CAS号17550-03-7 19-Norpregna-1,...

合成工艺路线路线简述

    雌酚酮置于potassium Tert-Butylate,Sodium Hydroxide体系中,用 四氢呋喃,水,丙酮 作为反应溶剂,化学反应 2.0H,反应生成 美雌醇
    参考文献:醋酸去甲孕甾醇的改进合成方法
    标题:醋酸去甲孕甾醇的改进合成方法
    摘要:口服避孕药(ocs)是合成类固醇或孕激素,在结构上与睾丸激素或孕激素有关.已经合成了许多孕激素并批准用于°C,激素替代疗法(hrt)或某些妇科疾病的治疗.醋酸诺美孕酮(nomac)是新批准的°C,并已在许多国家迅速接受oc或hrt.nomac的合成仍然具有挑战性且成本很高.我们开发了一种新颖且经过改进的合成nomac的方法,共11个步骤,并且在不使用危险试剂的情况下总体收率非常好.
    DOI:10.1021/op4003533

    海关参考信息

    专利信息


    专利号:US-7109377-B2
    优先权日:1996-10-16
    标 题:Synthesis of combinatorial libraries of compounds reminiscent of natural products
    发明人:SCHREIBER STUART L; SHAIR MATTHEW D; TAN DEREK S; FOLEY MICHAEL A; STOCKWELL BRENT R
    权利人:HARVARD COLLEGE
    摘要:The present invention provides complex compounds reminiscent of natural products and libraries thereof, as well as methods for their production. The inventive compounds and libraries of compounds are reminiscent of natural products in that they contain one or more stereocenters, and a high density and diversity of functionality. In general, the inventive libraries are synthesized from diversifiable scaffold structures, which are synthesized from readily available or easily synthesizable template structures. In certain embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from a shikimic acid based epoxyol template. In other embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from the pyridine-based template isonicotinamide. The present invention also provides a novel ortho-nitrobenzyl photolinker and a method for its synthesis. Furthermore, the present invention provides methods and kits for determining one or more biological activities of members of the inventive libraries. Additionally, the present invention provides pharmaceutical compositions containing one or more library members.

    专利号:US-4201869-A
    优先权日:1970-12-21
    标 题:Intermediates for steroid total synthesis process utilizing asymmetric induction
    发明人:COHEN NOAL; SAUCY GABRIEL
    权利人:HOFFMANN LA ROCHE
    摘要:A multi-step, stereospecific total synthesis of steroids is disclosed. The starting materials for this process are the relatively inexpensive and readily available m-alkoxy acetophenones. The process is suitable for the preparation of racemic or optically active, medicinally valuable steroids, particularly A-ring aromatic steroids. This process features an early optical resolution and a unique asymmetric induction which insures the correct stereochemistry of the final steroidal product.

    专利号:US-4092483-A
    优先权日:1973-10-16
    标题 :Intermediates for steroid total synthesis process utilizing asymmetric induction
    发明人:COHEN NOAL; SAUCY GABRIEL
    权利人:HOFFMANN LA ROCHE
    摘要:A multi-step, stereospecific total synthesis of steroids is disclosed. The starting materials for this process are the relatively inexpensive and readily available m-alkoxy acetophenones. The process is suitable for the preparation of racemic or optically active, medicinally valuable steroids, particularly A-ring aromatic steroids. This process features an early optical resolution and a unique asymmetric induction which insures the correct stereochemistry of the final steroidal product.

    专利号:US-4102925-A
    优先权日:1970-12-21
    标题:Steroid total synthesis process utilizing asymmetric induction
    发明人:COHEN NOAL; SAUCY GABRIEL
    权利人:HOFFMANN LA ROCHE
    摘要:A multi-step, stereospecific total synthesis of steroids is disclosed. The starting materials for this process are the relatively inexpensive and readily available m-alkoxy acetophenones. The process is suitable for the preparation of racemic or optically active, medicinally valuable steroids, particularly A-ring aromatic steroids. This process features an early optical resolution and a unique asymmetric induction which insures the correct stereochemistry of the final steroidal product.

    专利号:US-4011211-A
    优先权日:1973-10-16
    标题:Steroid total synthesis process utilizing asymmetric induction
    发明人:COHEN NOAL; SAUCY GABRIEL
    权利人:HOFFMANN LA ROCHE
    摘要:A multi-step, stereospecific total synthesis of steroids is disclosed. The starting materials for this process are the relatively inexpensive and readily available m-alkoxy aceto-phenones. The process is suitable for the preparation of racemic or optically active, medicinally valuable steroids, particularly A-ring aromatic steroids. This process features an early optical resolution and a unique asymmetric induction which insures the correct stereochemistry of the final steroidal product.

    专利号:US-2008300418-A1
    优先权日:2004-11-08
    标 题:Synthesis of Cardiolipin Analogues and Uses Thereof
    发明人:AHMAD MOGHIS U; UKKALAM MURALI K; ALI SHOUKATH M; AHMAD IMRAN
    权利人:AHMAD MOGHIS U; UKKALAM MURALI K; ALI SHOUKATH M; AHMAD IMRAN
    摘要:The invention provides novel synthetic methodologies for preparing cardiolipin, migrated caridiolipin (1,2-positional isomer of cardiolipin) and their analogues having varying fatty acids and/or alkyl chains with varying length and degrees of saturation/unsaturation. The method comprises (a) reacting an optically pure 1,2-O-dialkyl-sn-glycerol or 1,2-O-dialkyl-sn-glycerol with one or more phosphoramidite reagent(s), wherein a phosphite triester is produced; (b) coupling the product of (a) with glycerol, wherein a protected cardiolipin is produced; and (c) deprotecting the protected cardiolipin, such that cardiolipin is prepared. The cardiolipins and analogues thereof, prepared by the present methods, can be incorporated into liposomes, which can also include active agents such as hydrophobic or hydrophilic drugs, antisense nucleotides or diagnostic agents. Such liposomes can be used to treat diseases or can be used in diagnostic and/or analytical assays.
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    主要参考文献


    1: Hu JH, Wang L, Li WS, Dai DP, Cai JP, Hu GX. Effect of CYP2C9 Genetic Polymorphism in a Chinese Population on the Metabolism of Mestranol in vitro. Pharmacology. 2015;95(5-6):218-23. doi: 10.1159/000381189. Epub 2015 Apr 25. Polish. Japanese.
    10: Coezy E, Auzan C, Lonigro A, Philippe M, Menard J, Corvol P. Effect of mestranol on cell proliferation and angiotensinogen production in HepG2 cells: relation with the cell cycle and action of tamoxifen. Endocrinology. 1987 Jan;120(1):133-41. German. German.

    合成参考文献


    摘要:Chessum, N.; Couty, S.; Jones, K., Science of Synthesis, (2009) 48, 268.
    摘要:Kirk-Othmer Encyclopedia of Chemical Technology. 4th ed. Volumes 1: New York, NY. John Wiley and Sons, 1991-Present., p. V13 (96) 481
    摘要:Franke C et al; Chemosphere 29: 1501-14 (1994)
    摘要:S109 | PARCEDC | List of 7074 potential endocrine disrupting compounds (EDCs) by PARC T4.2 | DOI:10.5281/zenodo.10944198
    摘要:S72 | NTUPHTW | Pharmaceutically Active Substances from National Taiwan University | DOI:10.5281/zenodo.3955664
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