CAS: 75438-57-2; 4-Chloro-N-(4,5-Dihydro-1H-Imidazol-2-yl)-6-Methoxy-2-Methylpyrimidin-5-Amine

该化合物是一种主要用于治疗高血压的抗血压药物,它属于被称为imidazoline受体激动剂的药物类别,通过刺激大脑中特定的受体来调节血压而发挥作用.摩索尼丁的特点是对I1-免疫线受体采取选择性行动,导致同情性...

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CAS号75438-54-9 4,6-二氯-2-甲基-5-(... | CAS号67-56-1 甲醇 | CAS号287099-40-5 mono-Moxonidine... | CAS号124-41-4 甲醇钠 | CAS号438000-58-9 1-[1-((4,6-dich...

合成工艺路线路线简述

    盐酸莫索尼定置于base体系中,用 水 作为反应溶剂,化学反应生成 莫索尼啶
    参考文献:Synthesis Of Substituted Aminopyridines
    标题:Synthesis Of Substituted Aminopyridines
    摘要:本发明涉及一种用于制造具有化学式(i)的某些取代氨基吡啶的新型方法或其互变异构体或盐,其中r1从氢,卤素,C1-4烷氧基,C1-4烷硫基,C1-4烷基,C3-5环烷基中选择,例如r1为卤素如氯;r2为c1-4烷基,例如甲基,乙基,异丙基,正丙基或丁基(任何异构体),例如甲基;r3从氢,C1-4烷氧基,C1-4烷硫基,C1-4烷基,C3-5环烷基中选择,例如c1-4烷基如甲基,乙基,异丙基,正丙基或丁基(任何异构体),例如甲基;以及适用于执行该方法的化学中间体的结晶形式.

    海关参考信息

    专利信息


    专利号:US-9315483-B2
    优先权日:2007-09-13
    标题 :Synthesis of deuterated catechols and benzo[D][1,3]dioxoles and derivatives thereof
    发明人:JONES ANDREW D; ZELLE ROBERT E; SILVERMAN I ROBERT
    权利人:CONCERT PHARMACEUTICALS INC
    摘要:The present invention provides a convenient and efficient process for the synthesis of d 2 -benzo[d][1,3]dioxoles.

    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:WO-2015011010-A1
    优先权日:2013-07-26
    标 题:Synthesis of substituted aminopyrimidines
    发明人:ACQUASALIENTE MAURIZIO; LAGERWEIJ GERT; DESHPANDE MAHENDRA; SHAH RAJENDRA
    权利人:ABBOTT HEALTHCARE PRODUCTS BV; ABBOTT LAB
    摘要:The present invention relates to a novel process for the manufacture of certain substituted aminopyrimidines having Formula (I) or a tautomer or salt thereof, wherein R 1 is selected from hydrogen, halogen, C 1-4 alkoxy, C 1-4 alklthio, C 1-4 alkyl, C 3-5 cycloalkyl, for example R1 is halogen such as chloro; R2 is C 1-4 alkyl, for example methyl, ethyl, i-propyl, n-propyl or butyl (any isomer), such as methyl; and R3 is selected from hydrogen, C 1-4 alkoxy, C 1-4 alkylthio, C 1-4 alkyl, C 3-5 cycloalkyl, for example C 1-4 alkyl such as methyl, ethyl, i-propyl, n-propyl or butyl (any isomer), for example methyl; crystalline forms thereof as well as chemical intermediates suitable for use in performing the process.

    专利号:US-9018249-B2
    优先权日:2011-09-13
    标题 :SGLT inhibitors
    发明人:JAIN RAJESH; TREHAN SANJAY; DAS JAGATTARAN; NANDA GURMEET KAUR; THUNGATHURTHI SASTRY V R S; SINGH NISHAN; SHARMA SUDHIR KUMAR
    权利人:JAIN RAJESH; TREHAN SANJAY; DAS JAGATTARAN; NANDA GURMEET KAUR; THUNGATHURTHI SASTRY V R S; SINGH NISHAN; SHARMA SUDHIR KUMAR; PANACEA BIOTEC LTD
    摘要:The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to the processes for the synthesis of novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The present invention also provides pharmaceutical compositions comprising novel compounds of Formula I and methods of treating or preventing one or more conditions or diseases that may be regulated or normalized via inhibition of Sodium Glucose Cotransporter-2 (SGLT-2).

    专利号:US-2008039473-A1
    优先权日:2006-08-08
    标题:Preparation and utility of substituted quinazoline compounds with alpha-adrenergic blocking effects
    发明人:GANT THOMAS G; SARSHAR SEPEHR
    权利人:AUSPEX PHARMACEUTICALS INC
    摘要:The present disclosure is directed to modulators of alpha-adrenergic receptors and pharmaceutically acceptable salts and prodrugs thereof, the chemical synthesis thereof, and the use of such compounds for the treatment and/or management of hypertension, cardiac failure, prostatitis, and benign prostatic hyperplasia, and any other condition in which it is beneficial to modulate an alpha-adrenergic receptor.

    专利号:US-2014228303-A1
    优先权日:2011-06-13
    标题 :Novel sglt inhibitors
    发明人:JAIN RAJESH; TREHAN SANJAY; DAS JAGATTARAN; NANDA GURMEET KAUR; THUNGATHURTHI SASTRY V R S; SINGH NISHAN; SHARMA SUDHIR KUMAR
    权利人:JAIN RAJESH; TREHAN SANJAY; DAS JAGATTARAN; NANDA GURMEET KAUR; THUNGATHURTHI SASTRY V R S; SINGH NISHAN; SHARMA SUDHIR KUMAR; PANACEA BIOTEC LTD
    摘要:The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to the processes for the synthesis of novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The present invention also provides pharmaceutical compositions comprising novel compounds of Formula I and methods of treating or preventing one or more conditions or diseases that may be regulated or normalized via inhibition of Sodium Glucose Cotransporter-2 (SGLT-2).
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    主要参考文献


    1: Vasilenko AV, Melentyev AB, Dvorskaya ON. Razrabotka metodiki kolichestvennogo opredeleniya Moksonidina v krovi i moche metodom vysokoeffektivnoi zhidkostnoi khromatografii s tandemnym mass-selektivnym detektirovaniem [Development of a method for moxonidine quantification in blood and urine by high-performance liquid chromatography with tandem mass-selective detection]. Sud Med Ekspert. 2024;67(6):42-47. Russian. doi: 10.17116/sudmed20246706142. 64(8):24-31. Russian, English. doi: 10.18087/cardio.2024.8.n2731.
    29:10742484241258381. doi: 10.1177/10742484241258381. 42(12):2025-2040. doi: 10.1097/HJH.0000000000003769. Epub 2024 Sep 23.
    5: Tchernev G, Dimova D. PERIOCULAR HIGH RISK BCCS AFTER ADDITIONAL/PARALLEL INTAKE OF TORASEMIDE, MOXONIDINE AND MIRABEGRON: IMPORTANT LINKS TO SKIN CANCER RELATED (PHOTO-) NITROSOGENESIS IN THE CONTEXT OF PHARMACO-ONCOGENESIS. Georgian Med News. 2024 Feb;(347):70-76. 24(4):3857. doi: 10.3390/ijms24043857.

    合成参考文献


    摘要:Krupicka J, Soucek M, Chroust K. [The efficacy and safety of moxonidine in patients with metabolic syndrome (the O.B.E.Z.I.T.A. trial)]. Vnitr Lek. 2011 Jun;57(6):541–5.
    参考文献:10.2174/1874192401105010085
    摘要:Tziomalos K, Athyros VG, Karagiannis A, Mikhailidis DP. Dyslipidemia induced by drugs used for the prevention and treatment of vascular diseases. Open Cardiovasc Med J. 2011;5():85–9.
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