CAS: 81409-90-7; Cabergoline

该化合物是D2受体高度选择性的强效多巴胺受体激动剂. 它的主要治疗应用包括治疗超蛋白性贫血和帕金森病. 化合物的半衰期长,与其他通过谈判获得的激动剂相比,它可以减少剂量的频率. Cabergoline 的紧密结合和特殊性有助于它有效抑制蛋白分泌,使其成为管理蛋白质的首选. 此外,它的副作用发生率低,比如与溴丙烯相比,胃肠紊乱的发生率低,也提高了病人的合规性. 药物的稳定性和可预测的药性能进一步支持其在长期治疗疗法中的临床效用.

结构式图片

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C&L通报

上下游产品

CAS号153415-36-2 6-Norcabergoline | CAS号591-87-7 乙酸烯丙酯 | CAS号85329-86-8 去甲氨基甲酰基卡麦角林 | CAS号109-90-0 异氰酸乙酯 | CAS号25952-53-8 1-乙基-(3-二甲基氨基丙基... | CAS号81409-74-7 6-(2-丙烯基)二氢麦角酸 | CAS号1892-57-5 1-(3-二甲基氨基丙基)-3... | CAS号72821-79-5 6-(2-Propenyl)-... | CAS号72821-79-5 6-(2-Propenyl)-... | CAS号81409-74-7 6-(2-丙烯基)二氢麦角酸

合成工艺路线路线简述

  • 合成目标产物 Cabergoline 主要起始原料 Des-N-Allylcabergoline And Allyl Acetate
  • 85329-86-8 = 81409-90-7
    反应条件:1.1 Reagents: Triethylamine,Trimethylsilyl Triflate Solvents: Dichloromethane; -5 °C; 1 H,-5 - 0 °C; 24 H,18 - 20 °C1.2 24 H,15 - 20 °C1.3 Reagents: Tetrabutylammonium Fluoride Solvents: Tetrahydrofuran; 30 Min,0 - 5 °C; 1.5 H,0 - 5 °C
    标题:Process For Producing Cabergoline And Related Compounds And Novel Intermediates Therefor
    参考文献:Israel]

    474397-69-8 = 81409-90-7
    反应条件:1.1 Reagents: Hydrochloric Acid Solvents: Water1.2 Reagents: Ammonium Hydroxide Solvents: Water
    标题:A Practical Synthesis Of Cabergoline
    作者:Ashford,Scott W.; Et Al
    参考文献:Journal Of Organic Chemistry 日期:2002 卷标:67(20) 页码:7147-7150]

    474397-67-6 = 81409-90-7
    反应条件:1.1 Reagents: Triphenylphosphine,Cuprous Chloride Solvents: Dichloromethane; 20 H,35 - 40 °C; 40 °C -> 25 °C1.2 Reagents: Sodium Bicarbonate Solvents: Water; 20 Min,25 °C; 15 Min,25 °C1.3 Reagents: Hydrochloric Acid Solvents: Water; 1.5 H,75 - 80 °C1.4 Reagents: Ammonia Solvents: Ethyl Acetate,Water; Ph 10,25 °C
    标题:A Process For The Preparation Of Cabergoline
    作者:Chatterjee,Pranab; Et Al
    参考文献:Ip.Com Journal 日期:2007 卷标:7
(6Ar,9R,10Ar)-7-Allyl-4-(Tert-Butyldimethylsilyl)-N-(3-(Dimethylamino)Propyl)-N-(Ethylcarbamoyl)-4,6,6A,7,8,9,10,10A-octahydroindolo[4,3-Fg]Quinoline-9-Carboxamide置于氟化铵体系中,用 甲醇,水 作为反应溶剂,化学反应 3.0H,反应生成 卡麦角林
参考文献:Wo2006/97345
标题:Wo2006/97345

海关参考信息

专利信息


专利号:US-2012177593-A1
优先权日:2009-07-20
标 题 :Synthesis of dendrimer conjugates
发明人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH
权利人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH; UNIV MICHIGAN
摘要:The present invention relates to novel methods of synthesis of therapeutic and diagnostic dendrimers. In particular, the present invention is directed to novel dendrimer conjugates, novel methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer, inflammatory disease) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer conjugates of the present invention may further comprise at least two different components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy. Furthermore, the novel synthesis methods of certain embodiments of the present invention provide significant advantages with regard to total reaction time and simplicity.

专利号:WO-0054773-A1
优先权日:1999-03-12
标题:Dopamine agonists in combination with nitric oxide donors, compositions and methods of use
发明人:GARVEY DAVID S
权利人:NITROMED INC; GARVEY DAVID S
摘要:The present invention is directed to novel compositions comprising at least one dopamine agonist in combination with at least one nitric oxide donor (i.e. compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or are substrates for nitric oxide synthase). The novel compositions may optionally comprise at least one therapeutic agent, such as, a vasoactive agent, an antimetic agent, and mixtures thereof. The dopamine agonist is preferably apomorphine. The present invention is also directed to methods for treating and/or preventing sexual dysfunctions and/or enhancing sexual responses in patients. In other embodiments, the present invention is directed to methods treating or preventing neurodegenerative diseases, mitochondrial diseases, spinal cord injury, central or psychostimulant addiction, senile dementia, circulatory disorders, cardiovascular disorders, hyperprolactinaemia or myopia. The compounds and/or compositions of the present invention can also be provided in the form of a pharmaceutical kit.

专利号:US-9657030-B2
优先权日:2010-06-11
标 题 :Transition metal-catalyzed processes for the preparation of N-allyl compounds and use thereof
发明人:GIGUERE JOSHUA ROBERT; MCCARTHY KEITH EDWARD; REISCH HELGE ALFRED; SANDOVAL SERGIO; STYMIEST JAKE LARRY
权利人:RHODES TECH
摘要:The present disclosure provides processes for the N-dealkylation of tertiary amines and the use of transition metal catalysts to prepare tertiary N-allyl amine derivatives and secondary amine derivatives thereof. The tertiary amines can be alkaloids and, more particularly, the tertiary amines can be opioids. In specific embodiments, the present disclosure provides methods for use in processes for the synthesis of naloxone and naltrexone from oripavine.

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.

专利号:US-2015352230-A1
优先权日:2013-01-11
标 题:Synthesis and isolation of dendrimer based imaging systems
发明人:MULLEN DOUGLAS GURNETT; BAKER JR JAMES R; BANASZAK HOLL MARK M; HUANG BAOHUA; DOUGHERTY CASEY; BALL JACK
权利人:UNIV MICHIGAN
摘要:The present invention relates to novel methods of synthesis and isolation of antibodies conjugated with modular dendrimer nanoparticles. In particular, the present invention is directed to antibodies conjugated with novel modular dendrimer nanoparticles having precise numbers of imaging agents, methods of synthesizing the same, compositions comprising such antibodies conjugated with such modular dendrimer nanoparticles, as well as systems and methods utilizing the conjugates (e.g., in imaging settings) (e.g., in diagnostic and/or therapeutic settings) (e.g., for the delivery of therapeutics, imaging, and/or targeting agents).

专利号:US-2012232225-A1
优先权日:2009-08-26
标 题:Synthesis and isolation of dendrimer systems
发明人:BAKER JR JAMES R; BANASZAK HOLL MARK M; MULLEN DOUGLAS GURNETT; ORR BRADFORD G; DESAI ANKUR; SANDER LEONARD M; WADDELL JACK NEEL
权利人:BAKER JR JAMES R; BANASZAK HOLL MARK M; MULLEN DOUGLAS GURNETT; ORR BRADFORD G; DESAI ANKUR; SANDER LEONARD M; WADDELL JACK NEEL; UNIV MICHIGAN
摘要:The present invention relates to novel methods of synthesis and isolation of dendrimer systems. In particular, the present invention is directed to novel dendrimer conjugates with defined and limited numbers of ligand conjugates and high levels of structural uniformity, methods of synthesizing the same, compositions comprising the conjugates, as well systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer) diagnosis and/or therapy, pain therapy, etc.)).
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主要参考文献


1: Gadelha MR, Wildemberg LE, Shimon I. Pituitary acting drugs: cabergoline and pasireotide. Pituitary. 2022 Oct;25(5):722-725. doi: 10.1007/s11102-022-01238-8. Epub 2022 Jun 7. 185(4):D11-D20. doi: 10.1530/EJE-21-0344. 22(6):e25322. doi: 10.1002/jia2.25322.
4: Inder WJ, Jang C. Treatment of Prolactinoma. Medicina (Kaunas). 2022 Aug 13;58(8):1095. doi: 10.3390/medicina58081095.
5: Harris K, Murphy KE, Horn D, MacGilivray J, Yudin MH. Safety of Cabergoline for Postpartum Lactation Inhibition or Suppression: A Systematic Review. J Obstet Gynaecol Can. 2020 Mar;42(3):308-315.e20. doi: 10.1016/j.jogc.2019.03.014. Epub 2019 Jul 6. (2):CD008605. doi: 10.1002/14651858.CD008605.pub2. Update in: Cochrane Database Syst Rev. 2016 Nov 30;11:CD008605. 24(12):1238-1244. doi: 10.1177/1098612X221074924. Epub 2022 Feb 8. 123(45):1349-50. German. doi: 10.1055/s-0029-1237286. 38(8):868-80. doi: 10.1007/s00059-013-3816-0. Epub 2013 Jun 8. 101(3):664-75. doi: 10.1016/j.fertnstert.2013.11.005. Epub 2013 Dec 18. 2001(1):CD001518. doi: 10.1002/14651858.CD001518.

合成参考文献


参考文献:10.4274/jcrpe.v3i2.14
摘要:Eren E, Erdeve ŞS, Papatya Çakır ED, Ceylan LA, Sağlam H, Tarım Ö. Clinical Course of Hyperprolactinemia in Children and Adolescents: A Review of 21 Cases - Original Article. jcrpe. 2011 Jun 15;3(2):65–9. doi: 10.4274/jcrpe.v3i2.14.
参考文献:10.4103/0974-1208.82367
摘要:Singh P, Singh M, Cugati G, Singh AK. Bromocriptine or cabergoline induced pituitary apoplexy: Rare but life-threatening catastrophe. J Hum Reprod Sci. 2011 Jan;4(1):59.
参考文献:10.3389/fnsys.2011.00049
摘要:Collins-Praino LE, Paul NE, Rychalsky KL, Hinman JR, Chrobak JJ, Senatus PB, Salamone JD. Pharmacological and physiological characterization of the tremulous jaw movement model of parkinsonian tremor: potential insights into the pathophysiology of tremor. Front Syst Neurosci. 2011;5():49.
参考文献:10.1007/s00228-011-1084-6
摘要:Arbouw MEL, Movig KLL, Guchelaar H, Neef C, Egberts TCG. Dopamine agonists and ischemic complications in Parkinson’s disease: a nested case–control study. European Journal of Clinical Pharmacology. 2011 Jul 22;68(1):83–8. doi: 10.1007/s00228-011-1084-6.
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