CAS: 113775-47-6; Dexmedetomidine

该化合物是一种选择性的阿尔法-2肾上腺素激动剂,主要用于临床环境中的镇静剂和止痛剂特性,特别是在特护护理和外科手术期间;众所周知,它能够诱发镇静剂,而不会造成重大呼吸抑郁,因此它成为需要镇静剂的病人的首选,同时保持呼吸道反射;该化合物的半衰期相对较短,允许快速发作和抵消行动,这有利于需要快速康复的程序;Dexmetemetimedidine通常是静脉注射,其特点是其高脂溶性,有利于其在...

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CAS号576-23-8 3-溴邻二甲苯 | CAS号176721-02-1 (2,3-二甲基苯基)(1-三... | CAS号176721-01-0 ALPHA-(2,3-二甲基苯... | CAS号176721-03-2 1-(2,3-二甲基苯基)-1...

合成工艺路线路线简述

  • 合成目标产物 Dexmedetomidine 主要起始原料 Medetomidine
  • (文献来源)合成步骤主要原料 Medetomidine
4-<1-(2,3-Dimethylphenyl)-1-Hydroxyethyl>-1-(Triphenylmethyl)Imidazole置于palladium On Activated Charcoal 三乙基硅烷,氢气,三氟乙酸体系中,化学反应生成右美托咪定
参考文献:(S)-4(5)-[1-(2,3-二甲基苯基)乙基]咪唑酒石酸盐的有效合成,有效的α2肾上腺素受体激动剂右美托咪定
标题:(S)-4(5)-[1-(2,3-二甲基苯基)乙基]咪唑酒石酸盐的有效合成,有效的α2肾上腺素受体激动剂右美托咪定
摘要:摘要 (S,R)-4(5)-[1-(2,3-二甲基苯基)乙基]咪唑 5 以 41% 的收率通过一种新的可靠方法从易得的原料中制备.在 (R) 对映体游离碱的存在下,通过 (S) 对映体 6 的 (+/-)-酒石酸盐的选择性结晶进行对映体的分离.
Doi:10.1080/00397919608003527

海关参考信息

专利信息


专利号:US-6867202-B1
优先权日:1997-06-25
标 题 :Treatment of insulin resistance
发明人:CARPINO PHILIP ALBERT; CHIU CHARLES KWOK-FUNG; PAN LYDIA CODETTA; LEFKER BRUCE ALLEN; TREADWAY JUDITH LEE; ZAWISTOSKI MICHAEL PAUL
权利人:PFIZER
摘要:This invention is directed to methods of treating insulin resistance in a mammal which comprise administering an effective amount of a compound of formula I, n n nwhere the variables are defined in the specification, or the stereoisomeric mixtures, diastereomerically enriched, diastereomerically pure, enantiomerically enriched or enantiomerically pure isomers, or the pharmaceutically acceptable salts and prodrugs thereof to said mammal. The compounds of formula I are growth hormone secretagogues and as such are useful for increasing the level of endogenous growth hormone. In another aspect this invention provides certain intermediates which are useful in the synthesis of the foregoing compounds and certain processes useful for the synthesis of said intermediates and th compounds of formula I. This invention is further directed to methods comprising administering to a human or other animal a combination of a functional somatostatin antagonist such as an alpha-2 adrenergic agonist and a compound of formula I.

专利号:US-10053420-B2
优先权日:2015-01-30
标 题 :Processes for the preparation of compounds, such as 3-arylbutanals, useful in the synthesis of medetomidine
发明人:EKLUND LARS; EEK MARGUS; EKAMBARAM RAMESH; MAASALU ANTS
权利人:CAMBREX KARLSKOGA AB
摘要:There is provided a process for the preparation of a compound of formula (I) as defined herein, wherein said process comprises reacting a compound of formula (II) as defined s herein with one or more suitable Vilsmeier reagent.

专利号:WO-2025128098-A1
优先权日:2023-12-13
标 题 :Solid oral dosage forms, kits, and methods of using the same
发明人:LI YING; LANGER ROBERT; TRAVERSO CARLO
权利人:MASSACHUSETTS INST TECHNOLOGY; BRIGHAM & WOMENS HOSPITAL INC
摘要:Provided herein are solid oral dosage forms, methods, and kits useful, e.g, for the extension of the residence time of active pharmaceutical agents in vivo by the synthesis of a polymer in situ in a subject. In particular, the solid oral dosage forms, methods, and kits disclosed herein are particularly useful for drugs that require more than once daily administration (e.g, drugs that have short half-lives).

专利号:US-RE41998-E
优先权日:1990-02-26
标题 :Compositions and methods of treatment of sympathetically maintained pain
发明人:CAMPBELL JAMES N
权利人:ARCLON THERAPEUTICS INC
摘要:Sympathetically maintained pain is treated topically by administering to the site where sympathetically maintained pain is present an α-1-adrenergic antagonist, α-2-adrenergic agonist, or other drug that depletes or blocks synthesis of sympathetic norepinephrine, known collectively as sympatholytic agents. Chemical formulas for several sympatholytic agents are given.

专利号:US-6806291-B1
优先权日:2003-10-09
标 题:Analgesic compounds, their synthesis and pharmaceutical compositions containing them
发明人:SUNKEL CARLOS; ALVAREZ-BUILLA JULIO; BAZAN NICOLAS G; VACCARINO ANTHONY
权利人:FOUNDATION FOR THE LSU HEALTH
摘要:New analgesic compounds, which are prepared by the hydrolysis of N-acylated 4-hydroxyphenylamine derivatives, their synthesis and pharmaceutical compositions containing them are disclosed. These compounds surprisingly possess high analgesic activity with little hepatotoxic effect, making them more useful than conventional non-steroidal anti-inflammatory drugs (NSAIDs) in the treatment of chronic pain.

专利号:US-2019314312-A1
优先权日:2016-07-11
标题 :Combination therapy to increase endogenous nitric oxide (no) synthesis
发明人:EREZ AYELET; STETTNER NOA
权利人:YEDA RES & DEV
摘要:Provided are uses of a therapeutically effective amount of citrulline for the manufacture of a medicament for treatment of a subject having an inflammatory bowel disease (IBD) and/or colon cancer. Also provided are pharmaceutical compositions comprising a therapeutic effective amount of citrulline and a therapeutically effective amount of a flavonoid for the treatment of an inflammatory bowel disease (IBD) and/or colon cancer and kits comprising same.
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主要参考文献


1: Keating GM. Dexmedetomidine: A Review of Its Use for Sedation in the Intensive Care Setting. Drugs. 2015 Jul;75(10):1119-30. doi: 10.1007/s40265-015-0419-5. 43(12):1030-1040. doi: 10.1016/j.tips.2022.09.007. Epub 2022 Oct 21. 12(1):e0169525. doi: 10.1371/journal.pone.0169525.
4: Mondardini MC, Amigoni A, Cortellazzi P, Di Palma A, Navarra C, Picardo SG, Puzzutiello R, Rinaldi L, Vitale F, Zito Marinosci G, Conti G. Intranasal dexmedetomidine in pediatrics: update of current knowledge. Minerva Anestesiol. 2019 Dec;85(12):1334-1345. doi: 10.23736/S0375-9393.19.13820-5. Epub 2019 Oct 14. 62(1):118-33. doi: 10.1016/S0034-7094(12)70110-1. 69(8):487-492. doi: 10.1016/j.redare.2022.08.003. Epub 2022 Sep 10. 115(2):171-82. doi: 10.1093/bja/aev226. 40(1):111-130. doi: 10.1016/j.aan.2022.06.003. 18(10):64. doi: 10.1007/s11910-018-0873-z. Dexmedetomidine for Sepsis in Intensive Care Unit Randomized Evaluation (DESIRE) Trial Investigators. Effect of Dexmedetomidine on Mortality and Ventilator-Free Days in Patients Requiring Mechanical Ventilation With Sepsis: A Randomized Clinical Trial. JAMA. 2017 Apr 4;317(13):1321-1328. doi: 10.1001/jama.2017.2088.
11: Duan X, Coburn M, Rossaint R, Sanders RD, Waesberghe JV, Kowark A. Efficacy of perioperative dexmedetomidine on postoperative delirium: systematic review and meta-analysis with trial sequential analysis of randomised controlled trials. Br J Anaesth. 2018 Aug;121(2):384-397. doi: 10.1016/j.bja.2018.04.046. Epub 2018 Jun 22. 7(4):221-6. doi: 10.1097/00075198-200108000-00002. 64(9):947-961. English. doi: 10.1007/s12630-017-0917-x. Epub 2017 Jun 21. 45(2):345-353. doi: 10.1007/s11064-019-02922-1. Epub 2019 Dec 10. 78(3):371-380. doi: 10.1111/anae.15947. Epub 2022 Dec 19. 28(1):3-6. doi: 10.1097/EJA.0b013e32833e266d. 23(10):5452. doi: 10.3390/ijms23105452.

合成参考文献


摘要:Mountain BW, Smithson L, Cramolini M, Wyatt TH, Newman M. Dexmedetomidine as a pediatric anesthetic premedication to reduce anxiety and to deter emergence delirium. AANA J. 2011 Jun;79(3):219–24.
参考文献:10.1007/s12028-011-9588-6
摘要:Scaravilli V, Tinchero G, Citerio G; Participants in the International Multi-Disciplinary Consensus Conference on the Critical Care Management of Subarachnoid Hemorrhage. Fever management in SAH. Neurocrit Care. 2011 Sep;15(2):287–94. doi: 10.1007/s12028-011-9588-6.
参考文献:10.1159/000324554
摘要:Mizrak A, Erbagci I, Arici T, Avci N, Ganidagli S, Oner U. Dexmedetomidine use during strabismus surgery in agitated children. Med Princ Pract. 2011;20(5):427–32. doi: 10.1159/000324554.
参考文献:10.1186/1471-2474-12-163
摘要:Faensen B, Wildemann B, Hain C, Höhne J, Funke Y, Plank C, Stemberger A, Schmidmaier G. Local Application of BMP-2 Specific Plasmids in Fibrin Glue does not Promote Implant Fixation. BMC Musculoskeletal Disorders. 2011 Jul 15;12(1):163. doi: 10.1186/1471-2474-12-163.
摘要:Hu XG, Ruan XC, Yu L, Ding N, She SZ, Liao YL. [Effects of dexmedetomidine hydrochloride on ERK1/2 activation in a rat model of ventilator-induced lung injury]. Nan Fang Yi Ke Da Xue Xue Bao. 2011 Jun;31(7):1252–5.
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