CAS: 154323-57-6; Almotriptan

该化合物是一种选择性血清受体活性活性剂(5-HT1B/1D),主要用于急性治疗偏头痛和集束头痛,其机制包括收缩冠状血管血管和抑制阻燃性...

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上下游产品

3-(2-氨基乙基)-5-(1-吡咯烷磺酰基甲基)吲哚 3-(2-Aminoethyl)-5-(1-Pyrrolidinylsulfonylmethyl)Indole 181178-24-5
5-(1-Pyrrolidinylsulfonylmethyl)-3-Indolemethanol 334981-30-5
3-[2-(二甲基氨基)乙基]-5-[(1-吡咯烷基磺酰基)甲基]-1H-吲哚-1-甲醇 [3-[2-(Dimethylamino)Ethyl]-5-(Pyrrolidin-1-Ylsulfonylmethyl)Indol-1-Yl]Methanol 1018676-02-2
1-[[2-Carboxy-3-(2-Dimethylaminoethyl)-5-Indolyl]Methanesulphonyl]Pyrrolidine 154323-59-8
5-氯-N,N-二甲基色胺 5-Chloro-N,N-Dimethyltryptamine 22120-32-7
5-溴-N,N-二甲基色胺 5-Bromo-N,N-Dimethyltryptamine 17274-65-6

合成工艺路线路线简述

  • 合成目标产物 Almotriptan 主要起始原料 Pyrrolidine, 1-(Methylsulfonyl)- (9CI) And 5-Bromo-N,N-Dimethyltryptamine
  • (文献来源)合成步骤主要原料 Pyrrolidine, 1-(Methylsulfonyl)- (9Ci) 和 5-Bromo-N,N-Dimethyltryptamine
Almotriptan Succinate置于氨体系中,用 水,乙酸乙酯 用作溶剂,化学反应 0.5H,反应生成阿莫曲普坦
参考文献: Process For The Preparation Of 1-[[[3-[2-(Dimethylamino)Ethyl]-1H-Indol-5-Yl]Methyl]Sulfonyl] Pyrrolidine And Its Pharmaceutically Acceptable Salts[fr] Procede De Preparation De 1-[[[3-[2-(Dimethylamino)Ethyl]-1H-Indol-5-Yl]Methyl]Sulfonyl]Pyrrolidine Et De Ses Sels Pharmaceutiquement Acceptables
标题: Process For The Preparation Of 1-[[[3-[2-(Dimethylamino)Ethyl]-1H-Indol-5-Yl]Methyl]Sulfonyl] Pyrrolidine And Its Pharmaceutically Acceptable Salts[fr] Procede De Preparation De 1-[[[3-[2-(Dimethylamino)Ethyl]-1H-Indol-5-Yl]Methyl]Sulfonyl]Pyrrolidine Et De Ses Sels Pharmaceutiquement Acceptables

海关参考信息

专利信息


专利号:US-8822702-B2
优先权日:2002-12-20
标 题 :Synthesis of amines and intermediates for the synthesis thereof
发明人:BERENS ULRICH; DOSENBACH OLIVER; SPRENGER DANIEL
权利人:BERENS ULRICH; DOSENBACH OLIVER; SPRENGER DANIEL; BASF SE
摘要:The invention relates in a first embodiment to a method for the manufacture of esters of the formula I, n nor especially of amides of the formula II,n n nwherein the symbols have the meanings given in the specification, as well as other intermediates and compounds useful in the synthesis of tryptamines and other substances mentioned in the title. The synthesis methods and intermediates are useful in the synthesis of pharmaceuticals.

专利号:US-2025188502-A1
优先权日:2022-03-10
标 题 :Biocatalyst and method for the synthesis of ubrogepant intermediates
发明人:CHEN HAIBIN; HU HU; CAI BAOQIN; XU JUNPENG; LIU SITONG; JIN LUPING; WU XINWEI; CUI QINYAN; ZHANG CHENGXIAO; ZHU KAILONG
权利人:ENZYMASTER NINGBO BIO ENG CO LTD
摘要:This application provides engineered transaminase polypeptides for the synthesis of Ubrogepant intermediates with high stereoselectivity, high catalytic activity and good stability. This application also provides a reaction process for the asymmetric synthesis of Ubrogepant intermediates using the transaminase polypeptide.

专利号:US-8304409-B2
优先权日:2002-07-03
标 题:Nitrosated nonsteroidal antiinflammatory compounds, compositions and methods of use
发明人:EARL RICHARD A; EZAWA MAIKO; FANG XINQIN; GARVEY DAVID S; GASTON RICKY D; KHANAPURE SUBHASH P; LETTS L GORDON; LIN CHIA-EN; RANATUNGE RAMANI R; RICHARDSON STEWART K; SCHROEDER JOSEPH D; STEVENSON CHERI A; WEY SHIOW-JYI
权利人:EARL RICHARD A; EZAWA MAIKO; FANG XINQIN; GARVEY DAVID S; GASTON RICKY D; KHANAPURE SUBHASH P; LETTS L GORDON; LIN CHIA-EN; RANATUNGE RAMANI R; RICHARDSON STEWART K; SCHROEDER JOSEPH D; STEVENSON CHERI A; WEY SHIOW-JYI; NICOX SA
摘要:The invention describes novel nitrosated nonsteroidal antiinflammatory drugs (NSAIDs) and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated NSAID, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one nitrosated NSAID, and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one nitrosated NSAID, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating inflammation, pain and fever; for treating gastrointestinal disorders; for facilitating wound healing; for treating and/or preventing gastrointestinal, renal and/or respiratory toxicities resulting from the use of nonsteroidal antiinflammatory compounds; for treating inflammatory disease states and/or disorders; and for treating and/or preventing ophthalmic diseases and/or disorders.

专利号:US-2002183366-A1
优先权日:2001-03-23
标题:Cyclooxygenase-2 inhibitors, compositions and methods of use
发明人:GARVEY DAVID S; SCHROEDER JOSEPH D
摘要:This invention describes novel compounds that are cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or, optionally, at least one therapeutic agent. The invention also provides novel kits comprising at least one COX-2 selective inhibitor, and, optionally, at least one nitric oxide donor, and/or, optionally, at least one therapeutic agent. The novel cyclooxygenase 2 selective inhibitors of the invention can be optionally nitrosated and/or nitrosylated. The invention also provides methods for treating inflammation, pain and fever; for treating and/or improving the gastrointestinal properties of COX-2 selective inhibitors; for facilitating wound healing; for treating and/or preventing renal toxicity or other toxicities; for treating and/or preventing other disorders resulting from elevated levels of cyclooxygenase-2; and for improving the cardiovascular profile of COX-2 selective inhibitors.

专利号:US-7211598-B2
优先权日:2002-06-28
标 题:Oxime and/or hydrozone containing nitrosated and/or nitrosylated cyclooxygenase-2 selective inhibitors, compositions and methods of use
发明人:GARVEY DAVID S; RANATUNGE RAMANI R; RICHARDSON STEWART K
权利人:NITROMED INC
摘要:The invention describes novel cyclooxygenase 2 (COX-2) selective inhibitors having at least one oxime group or hydrazone group and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor having at least one oxime group or hydrazone group, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one COX-2 selective inhibitor having at least one oxime group or hydrazone group, optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor, and/or, optionally, at least one therapeutic agent. The novel cyclooxygenase 2 selective inhibitors of the invention having at least one oxime group or hydrazone group can be optionally nitrosated and/or nitrosylated. The invention also provides methods for treating inflammation, pain and fever; for treating and/or improving the gastrointestinal properties of COX-2 selective inhibitors; for facilitating wound healing; for treating and/or preventing renal and/or respiratory toxicity; for treating and/or preventing other disorders resulting from elevated levels of cyclooxygenase-2; and for improving the cardiovascular profile of COX-2 selective inhibitors.

专利号:US-6825185-B2
优先权日:2000-12-21
标题:Substituted aryl compounds as novel cyclooxygenase-2 selective inhibitors, compositions and methods of use
发明人:KHANAPURE SUBHASH P; GARVEY DAVID S; EARL RICHARD A; EZAWA MAIKO; FANG XINQIN; GASTON RICKY D
权利人:NITROMED INC
摘要:The invention describes novel substituted aryl compounds that are cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or, optionally, at least one therapeutic agent, such as, steroids, nonsterodal antiinflammatory compounds (NSAID), 5-lipoxygenase (5-LO) inhibitors, leukotriene B 4 (LTB 4 ) receptor antagonists, leukotriene A 4 (LTA 4 ) hydrolase inhibitors, 5-HT agonists, 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) inhibitors, H 2 antagonists, antineoplastic agents, antiplatelet agents, thrombin inhibitors, thromboxane inhibitors, decongestants, diuretics, sedating or non-sedating anti-histamines, inducible nitric oxide synthase inhibitors, opioids, analgesics, Helicobacter pylori inhibitors, proton pump inhibitors, isoprostane inhibitors, and mixtures thereof. The invention also provides novel kits comprising at least one COX-2 selective inhibitor, and, optionally, at least one nitric oxide donor, and/or, optionally, at least one therapeutic agent. The novel cyclooxygenase 2 selective inhibitors of the invention can be optionally nitrosated and/or nitrosylated. The invention also provides methods for treating inflammation, pain and fever; for treating and/or improving the gastrointestinal properties of COX-2 selective inhibitors; for facilitating wound healing; for treating and/or preventing renal toxicity or other toxicities; for treating and/or preventing other disorders resulting from elevated levels of cyclooxygenase-2; and for improving the cardiovascular profile of COX-2 selective inhibitors.
江苏省金坛市兢业医化技术研究所
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主要参考文献


1: Abbas Z, Marihal S. Gellan gum-based mucoadhesive microspheres of almotriptan for nasal administration: Formulation optimization using factorial design, characterization, and in vitro evaluation. J Pharm Bioallied Sci. 2014 Oct;6(4):267-77. doi: 10.4103/0975-7406.142959.
2: Orlandini S, Pasquini B, Stocchero M, Pinzauti S, Furlanetto S. An integrated quality by design and mixture-process variable approach in the development of a capillary electrophoresis method for the analysis of almotriptan and its impurities. J Chromatogr A. 2014 Apr 25;1339:200-9. doi: 10.1016/j.chroma.2014.02.088. Epub 2014 Mar 12. doi: 10.5681/apb.2013.030. Epub 2013 Feb 7.
5: Nirogi R, Ajjala DR, Kandikere V, Aleti R, Pantangi HR, Srikakolapu SR, Benade V, Bhyrapuneni G, Vurimindi H. LC-MS/MS method for the quantification of almotriptan in dialysates: application to rat brain and blood microdialysis study. J Pharm Biomed Anal. 2013 Jul-Aug;81-82:160-7. doi: 10.1016/j.jpba.2013.04.008. Epub 2013 Apr 16. doi: 10.1517/17425255.2013.783012. Epub 2013 Apr 9. doi: 10.3797/scipharm.1112-01. Epub 2012 Feb 27.

合成参考文献


参考文献:10.2165/11590370-000000000-00000
摘要:Källén B, Nilsson E, Otterblad Olausson P. Delivery outcome after maternal use of drugs for migraine: a register study in Sweden. Drug Saf. 2011 Aug 01;34(8):691–703. doi: 10.2165/11590370-000000000-00000.
参考文献:10.3109/00207454.2011.605191
摘要:Díaz-Insa S, Goadsby PJ, Zanchin G, Fortea J, Falqués M, Vila C. The Impact of Allodynia on the Efficacy of Almotriptan When Given Early in Migraine: Data From the “Act When Mild” Study. International Journal of Neuroscience. 2011 Aug 22;121(12):655–61. doi: 10.3109/00207454.2011.605191.
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