CAS: 84057-84-1; 6-(2,3-Dichlorophenyl)-1,2,4-Triazine-3,5-Diamine

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CAS号84689-20-3 2-(2,3-二氯苯基)-2-... | CAS号6574-97-6 2,3-二氯苯腈 | CAS号2582-30-1 氨基胍碳酸氢盐 | CAS号77668-42-9 2,3-二氯苯甲酰氰 | CAS号71-23-8 正丙醇 | CAS号879573-84-9 6-(2,3-dichloro... | CAS号32768-54-0 2,3-二氯甲苯 | CAS号57915-78-3 2,3-二氯苄溴

合成工艺路线路线简述

  • 130801-01-3 + 4418-61-5 = 84057-84-1
    反应条件:1.1 Reagents: Sodium Nitrite,Hydrochloric Acid Solvents: Water; 30 Min,-2 °C1.2 Reagents: Sodium Acetate Solvents: Ethanol,Water; 2 H,Rt1.3 Solvents: Acetic Acid; Reflux2.1 Reagents: Copper Solvents: Acetic Acid; 2 H,Reflux2.2 Reagents: Ammonia Solvents: Water
    标题:A New Approach To The Synthesis Of Lamotrigine And Other 3,5-Diamino-1,2,4-Triazine Derivatives
    作者:Ulomskii,E. N.; Et Al
    参考文献:Russian Chemical Bulletin 日期:2005 卷标:54(3) 页码:726-732]

    79-17-4 + 491832-35-0 + 463-79-6 = 84057-84-1
    反应条件:1.1 Reagents: Hydrochloric Acid Solvents: Water; Rt1.2 Rt1.3 Reagents: Sodium Hydroxide Solvents: Water; Rt2.1 Solvents: Dimethylformamide; 20 H2.2 Solvents: Isopropanol2.3 Reagents: Sodium Hydroxide Solvents: Water
    标题:Process For The Preparation Of Lamotrigine Via Cyclization Of Oxodichlorophenylacetamidine
    参考文献:Hungary]

    = 84057-84-1
    反应条件:1.1 Solvents: Dimethylformamide; 20 H1.2 Solvents: Isopropanol1.3 Reagents: Sodium Hydroxide Solvents: Water
    标题:Process For The Preparation Of Lamotrigine Via Cyclization Of Oxodichlorophenylacetamidine
    参考文献:Hungary]

    84689-20-3 = 84057-84-1
    反应条件:1.1 Solvents: Methanol; 2 H,Reflux; 15 Min,63 - 65 °C; 15 H,Reflux
    标题:Process For Producing 6-(2,3-Dichlorophenyl)-1,2,4-Triazine-3,4-Diamine (Lamotrigine) And Identification,Characterization Of A New N-Methyl Impurity
    作者:Venkanna,G.; Et Al
    参考文献:Pharma Chemica 日期:2012 卷标:4(1) 页码:100-105]

    79-17-4 + 463-79-6 + 77668-42-9 = 84057-84-1
    反应条件:1.1 Reagents: Nitric Acid Solvents: Water; 30 Min,25 °C1.2 Solvents: Dimethyl Sulfoxide; 25 °C; 3 H,25 °C; 7 D,Rt1.3 Reagents: Ammonium Hydroxide Solvents: Water; Ph 12; 30 Min,Cooled1.4 Reagents: Potassium Hydroxide Solvents: Methanol; 12 H,Reflux1.5 Reagents: Water; 30 Min,Cooled
    标题:Synthesis Of 6-(2,3-Dichlorophenyl)-1,2,4-Triazine-3,5-Diamine (Lamotrigine)
    作者:Deng,Hong; Et Al
    参考文献:Zhongguo Yiyao Gongye Zazhi 日期:2006 卷标:37(10) 页码:657-658]

    879573-84-9 = 84057-84-1
    反应条件:1.1 Reagents: Copper Solvents: Acetic Acid; 2 H,Reflux1.2 Reagents: Ammonia Solvents: Water
    标题:A New Approach To The Synthesis Of Lamotrigine And Other 3,5-Diamino-1,2,4-Triazine Derivatives
    作者:Ulomskii,E. N.; Et Al
    参考文献:Russian Chemical Bulletin 日期:2005 卷标:54(3) 页码:726-732]

    79-17-4 + 77668-42-9 = 84057-84-1 [标题:Reaction Conditions
    标题:An Evaluation Of Multiple Catalytic Systems For The Cyanation Of 2,3-Dichlorobenzoyl Chloride: Application To The Synthesis Of Lamotrigine
    作者:Leitch,David C.; Et Al
    参考文献:Organic Process Research & Development 日期:2017 卷标:21(11) 页码:1815-1821]

    79-17-4 + 77668-42-9 = 84057-84-1
    反应条件:1.1 Reagents: Sulfuric Acid Solvents: Water; 6 H,55 °C2.1 Solvents: Methanol; 2 H,65 °C
    标题:Digitization Of Multistep Organic Synthesis In Reactionware For On-Demand Pharmaceuticals
    作者:Kitson,Philip J.; Et Al
    参考文献:Science (Washington 日期:2018 卷标:359(6373) 页码:314-319]

    1937-19-5 + 77668-42-9 = 84057-84-1
    反应条件:1.1 Reagents: Methanesulfonic Acid Solvents: Dimethylformamide; 1 H,Rt1.2 Solvents: Dimethylformamide; Rt -> 60 °C; 2.5 H,60 °C; Cooled1.3 Reagents: Sodium Hydroxide Solvents: Water; Ph 12,Cooled2.1 Reagents: Potassium Hydroxide Solvents: Isopropanol; Rt; Rt -> 105 °C; 6 H,105 °C2.2 Reagents: Hydrochloric Acid Solvents: Water; Ph 7
    标题:Synthesis And Antimicrobial Activity Of Lamotrigine And Its Ammonium Derivatives
    作者:Qian,Yong; Et Al
    参考文献:Journal Of Chemical Sciences (Bangalore 日期:2009 卷标:121(4) 页码:463-470
在 Sodium Hydroxide体系中,化学反应 3.0H,以97%的收率获得产物那蒙特金
参考文献:一种改进的拉莫三嗪合成工艺
标题:一种改进的拉莫三嗪合成工艺
摘要:本发明公开了一种改进的拉莫三嗪合成工艺,包括以下步骤:(1)2,3‑二氯苯甲酰氰合成:于反应器中投加2,3‑二氯苯甲酸,氯化亚砜,反应完成减压蒸净氯化亚砜,投加氰化亚铜,反应完成后滤除固体,得2,3‑二氯苯甲酰氰溶液;(2)缩合物制备:于反应器中加入氨基胍碳酸盐及共沸剂,滴加浓硫酸,蒸出共沸剂,并带出水,抽滤,固体进反应瓶,减压抽干后加入步骤1得到的2,3‑二氯苯甲酰氰溶液,反应完成后降至室温,抽滤,得缩合物;(3)环合物制备:步骤2得到的缩合物中加入液碱,反应后析晶,过滤,洗涤,烘干得拉莫三嗪.本发明可显著提高产物拉莫三嗪的品质及收率,收率达90%以上.

海关参考信息

专利信息


专利号:US-7390899-B2
优先权日:2002-09-20
标 题:Process for the synthesis of high purity 3,5-diamino-6-(2,3-dichlorophenyl) (1,2,4-triazine)
发明人:NEU JOZSEF; GIZUR TIBOR; TOERLEY JOZSEF; CSABAI JANOS; VEGH FERENC; KALVIN PETER; TARKANYI GABOR
权利人:RICHTER GEDEON VEGYESZET
摘要:The present invention relates to a new process for the synthesis of high purity 3,5-diamino-6-(2,3-dichlorophenyl)-1,2,4-triazine of formula (I) using 2,3-dichlorobenzoyl cyanide and an aminoguanidine salt as starting materials. 2,3-dichlorobenzoyl cyanide is reacted with 1-2 mol equivalent of aminoguanidine salt in 3-6 mol equivalent of methanesulfonic acid, then the obtained adduct of formula (IV) is transformed without isolation into the product with magnesium oxide. In given case the obtained crude product can be recrystallized from a proper organic solvent

专利号:US-10022446-B2
优先权日:2014-08-22
标题 :PH responsive hybrid hydrogel and method of synthesis thereof
发明人:KIZILEL SEDA; CEVIK OZLEM
权利人:KOC UENIVERSITESI
摘要:A pH-responsive hybrid hydrogel, namely poly(Methacrylic acid-grafted-Ethylene Glycol) P(MAA-g-EG) cross-linked with Styrene-Butadiene-Styrene (SBS) polymer and photopolymerized by visible light. The resulting polymer turned out to have better integrities, high swelling ratios, pH-responsive and biocompatible character. Also the visible-light-induced synthesis of these pH-responsive composite wherein eosin Y is used as photoinitiator and triethanolamine is used as a co-initiator is also disclosed in the invention.

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:WO-2016028237-A1
优先权日:2014-08-22
标题 :A novel ph responsive hydrogel and method of synthesis
发明人:KIZILEL SEDA; CEVIK OZLEM
权利人:KOÇ ÜNIVERSITESI
摘要:A pH-responsive hydrogel, namely poly(Methacrylic acid-grafted-Ethylene Glycol) P(MAA-g-EG), that is synthesized via photopolymerization that is initiated by visible light with enhanced swelling properties as compared to P(MAA-g-EG) hydrogel that is synthesized through UV-light initiated photopolymerization technique. Also the method of synthesis of the said hydrogel and the use of the hydrogel in pharmacy for drug delivery applications.

专利号:US-2024417358-A1
优先权日:2021-10-04
标题:Continuous Flow Reactor and Process for Synthesis of Substituted Benzoic Acid
发明人:JOSHI SUNIL SHANKAR; MALI NILESH ATMARAM
权利人:COUNCIL SCIENT IND RES
摘要:The present invention provides a non-hazardous, improved continuous oxidation process for the preparation of substituted benzoic acid of formula (I) by using continuous process reactor system with improved process controls. (I) wherein: R 1 is H, F, Cl, Br, I, NO 2 , amine, or C 1 -C 5 alkyl; R 2 is H, F, Cl, Br, I, NO 2 , amine, or C 1 -C 5 alkyl; and R 3 is H, F, Cl, Br, I, NO 2 , amine, C 1 -C 5 alkyl;

专利号:US-8207221-B2
优先权日:2004-01-30
标 题:Crystalline polymorphs of a CXC-chemokine receptor ligand
发明人:HU MENGWEI; YU YOUNONG; DWYER MICHAEL P; TAVERAS ARTHUR G; KIM-MEADE AGNES; YIN JIANGUO; FU XIAOYONG; MCALLISTER TIMOTHY L; ZHANG SHUYI; KLOPFER KEVIN
权利人:HU MENGWEI; YU YOUNONG; DWYER MICHAEL P; TAVERAS ARTHUR G; KIM-MEADE AGNES; YIN JIANGUO; FU XIAOYONG; MCALLISTER TIMOTHY L; ZHANG SHUYI; KLOPFER KEVIN; SCHERING CORP
摘要:The present invention relates to four distinct crystalline polymorphs of a monohydrate of Compound A having the following chemical structure: n n n n n n n n n n These four polymorphic forms, herein referred to as Forms I, II, III and IV are active as a CXC-chemokine receptor ligands. The invention is further directed to formulations, methods of treatment, and processes of synthesis of these polymorphic forms.
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主要参考文献


1: Soysal H, Doğan Z, Kamışlı Ö. Effects of phenytoin and lamotrigine treatment on serum BDNF levels in offsprings of epileptic rats. Neuropeptides. 2015 Dec 8. pii: S0143-4179(15)00221-8. doi: 10.1016/j.npep.2015.12.001. [Epub ahead of print] Review. doi: 10.1136/bmjopen-2015-007711. Review.
3: Wang XQ, Xiong J, Xu WH, Yu SY, Huang XS, Zhang JT, Tian CL, Huang DH, Jia WQ, Lang SY. Risk of a lamotrigine-related skin rash: current meta-analysis and postmarketing cohort analysis. Seizure. 2015 Feb;25:52-61. doi: 10.1016/j.seizure.2014.12.001. Epub 2014 Dec 23. Review. doi: 10.3389/fphar.2015.00242. eCollection 2015. Review.
5: Sinclair S, Cunnington M, Messenheimer J, Weil J, Cragan J, Lowensohn R, Yerby M, Tennis P. Advantages and problems with pregnancy registries: observations and surprises throughout the life of the International Lamotrigine Pregnancy Registry. Pharmacoepidemiol Drug Saf. 2014 Aug;23(8):779-86. doi: 10.1002/pds.3659. Epub 2014 Jun 27. Review.

合成参考文献


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摘要:Broli M, Provini F, Naldi I, Bisulli F, Sama C, Baruzzi A, Tinuper P, Riva R. Unexpected gamma glutamyltransferase rise increase during levetiracetam monotherapy. Epileptic Disord. 2010 Mar;12(1):81–2. doi: 10.1684/epd.2010.0291.
参考文献:10.1016/j.ridd.2011.06.007
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摘要:Mula M, Hesdorffer DC. Suicidal behavior and antiepileptic drugs in epilepsy: analysis of the emerging evidence. Drug Healthc Patient Saf. 2011;3():15–20.
参考文献:10.1016/j.jocn.2011.02.018
摘要:Manohar C, Avitsian R, Lozano S, Gonzalez-Martinez J, Cata JP. The effect of antiepileptic drugs on coagulation and bleeding in the perioperative period of epilepsy surgery: The Cleveland Clinic experience. Journal of Clinical Neuroscience. 2011 Sep;18(9):1180–4. doi: 10.1016/j.jocn.2011.02.018.
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