CAS: 59-63-2; N'-Benzyl-5-Methylisoxazole-3-Carbohydrazide

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CAS号19788-35-3 5-甲基异恶唑-3-羧酸甲酯 | CAS号20570-96-1 苄基肼二盐酸盐 | CAS号91397-11-4 5-Methyl-3-isox... | CAS号62438-03-3 5-甲基异唑-3-甲酸酐 | CAS号100-52-7 苯甲醛 | CAS号555-96-4 苄基肼 | CAS号491594-42-4 2-benzyl-4-(2-o...

合成工艺路线路线简述

  • 合成目标产物 Isocarboxazid (200 Mg) 主要起始原料 Methyl 5-Methylisoxazole-3-Carboxylate And Benzylhydrazine Dihydrochloride
  • (文献来源)合成步骤主要原料 Methyl 5-Methylisoxazole-3-Carboxylate 和 Benzylhydrazine Dihydrochloride
📜5-甲基异唑-3-甲酸酐置于钾硼氢体系中,用 甲醇,乙醇,水 作为反应溶剂,化学反应生成 异卡波肼
参考文献:单胺氧化酶抑制剂.i.1-烷基和1-芳烷基-2-(吡啶啉基和5-甲基-3-异恶唑基-羰基)肼.
标题:单胺氧化酶抑制剂.i.1-烷基和1-芳烷基-2-(吡啶啉基和5-甲基-3-异恶唑基-羰基)肼.
摘要:
DOI:10.1021/jm50009A002

海关参考信息

专利信息


专利号:US-7576211-B2
优先权日:2004-09-30
标题 :Synthesis of thienopyridinone compounds and related intermediates
发明人:DHANOA DALE S; BECKER OREN; NOIMAN SILVIA; CHEN DONGLI; MARANTZ YAEL; SHACHAM SHARON; HEIFETZ ALEXANDER; INBAL BOAZ; BAR-HAIM SHAY; MOHANTY PRADYUMNA; LOBERA MERCEDES; WU LAURENCE
权利人:EPIX DELAWARE INC
摘要:The invention relates to 5-HT receptor agonists and partial agonists. Novel thienopyridinone compounds represented by Formula I, and synthesis and uses thereof for treating diseases mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include Alzheimer's disease, cognition disorders, irritable bowel syndrome, nausea, emesis, vomiting, prokinesia, gastroesophageal reflux disease, nonulcer dyspepsia, depression, anxiety, urinary incontinence, migraine, arrhythmia, atrial fibrillation, ischemic stroke, gastritis, gastric emptying disorders, feeding disorders, gastrointestinal disorders, constipation, erectile dysfunction, and respiratory depression. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.

专利号:US-4310535-A
优先权日:1976-11-30
标题:Combination of drugs and a method for the selective control of the immune reactions evoked in a host by the administration of antigens
发明人:PIERPAOLI WALTER
权利人:PIERPAOLI WALTER
摘要:The invention concerns a new composition or combination of drugs effective to selectively control the immune reactions which are evoked in a host by the administration of antigens. It comprises active components capable of simultaneously blocking the alpha -adrenergic receptors of the cells for catecholamine, blocking the dopaminergic receptors of the cells and increasing the synthesis of serotonin. Preferred drug combinations according to the invention contain in association phentolamine, haloperidol, L-5-hydroxy-tryptophane and possibly dopamine.

专利号:US-2005080260-A1
优先权日:2003-04-22
标 题 :Preparation of prodrugs for selective drug delivery
发明人:MILLS RANDELL L; WU GUO-ZHANG
摘要:Synthesis of a chemical compound having the formula A-B-C that may serve for applications such as drug delivery where A is a chemiluminescent, moiety, B is a photochromic moiety, and C is a biologically active moiety where A-B-C may serve as a prodrug. Novel synthetic methods of the present invention to form the prodrug comprised the steps of (1) forming a benzophenone, (2) forming a diaryl ethylene, (3) attaching a phthalimide moiety to at least one of the aryl groups of the ethylene to form a phthalimide-ethylene conjugate, (4) condensing two ethylene-phthalimide conjugates to form a phthalimide-pentadiene conjugate, (5) converting the phthalimide to the phthalhydrazide by reaction with hydrazine to form a carrier compound according to the present invention, and (6) reacting the carrier compound with an nucleophilic moiety of the drug to form the corresponding prodrug. Alternatively the carrier can be prepared by using the halo-substituted diaryl ethylene to make the corresponding cationic leuco dye-like compound with known methods. The cationic compound then is protected by reacting with a nucleophile and coupled with the aminophathalimide by palladium-catalyzed amination to form the protected phthalimide-pentadiene conjugate. The latter is refluxed with hydrazine to convert its phthalimide to the phthalhydrazide and acidified to give the carrier. An additional aspect of the present invention relates to the use of these compounds as antiviral agents for the treatment of viral infections such as HIV and as anticancer agents for the treatment of cancers such as bowel, lung, and breast cancer.

专利号:US-2008214827-A1
优先权日:2004-02-03
标 题:Synthesis of Cyanoimino-Benzoimidazoles
发明人:GOEHRING R RICHARD; WHITEHEAD JOHN; SHAO BIN
权利人:EURO CELTIQUE SA
摘要:Disclosed in certain embodiments is a process for synthesizing a compound of formula (V) and salts thereof.

专利号:US-10329264-B2
优先权日:2015-07-31
标题 :Process for the preparation of isocarboxazid
发明人:DE FAVERI CARLA; HUBER FLORIAN ANTON MARTIN; ANTOLINI NICOLA
权利人:LUNDBECK PHARMACEUTICALS ITALY S P A
摘要:This invention relates to a novel chemical process for the synthesis of N′-benzyl-5-methylisoxazole-3-carbohydrazide (Isocarboxazid) which comprises reacting 5-methyl-3-isoxazole carboxylic acid ester with benzylhydrazine or a salt thereof in an aprotic organic solvent and in the presence of an organic base.

专利号:US-6787668-B2
优先权日:2000-04-13
标 题 :2-amino-4,5 heptenoic acid derivatives useful as nitric oxide synthase inhibitors
发明人:PITZELE BARNETT S; SIKORSKI JAMES A; WEBBER RONALD KEITH
权利人:PHARMACIA CORP
摘要:The present invention is directed to a compound of formula I:or a pharmaceutically acceptable salt thereof, wherein:R1 is selected from the group consisting of H and methyl; andR2 is selected from the group consisting of H and methyl.The compounds possess useful nitric oxide synthetase inhibiting activity, and are expected to be useful in the treatment or prophylaxis of a disease or condition in which the synthesis or over synthesis of nitric oxide forms a contributory part.

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主要参考文献


1: Larsen JK, Bendsen BB, Bech P. Vitamin B6 treatment of oedema induced by mirtazapine and isocarboxazid. Acta Psychiatr Scand. 2011 Jul;124(1):76-7; discussion 77. doi: 10.1111/j.1600-0447.2011.01695.x. Epub 2011 Mar 16.

合成参考文献


参考文献:10.1007/s00535-005-1687-8
摘要:Hojo M, Miwa H, Yokoyama T, Ohkusa T, Nagahara A, Kawabe M, Asaoka D, Izumi Y, Sato N. Treatment of functional dyspepsia with antianxiety or antidepressive agents: systematic review. J Gastroenterol. 2005 Nov;40(11):1036–42. doi: 10.1007/s00535-005-1687-8.
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