CAS: 863031-21-4; (5-Methyl-2-Oxo-1,3-Dioxol-4-yl)Methyl 2-Ethoxy-1-((2'-(5-Oxo-4,5-Dihydro-1,2,4-Oxadiazol-3-yl)-[1,1'-Biphenyl]-4-yl)Methyl)-1H-Benzo[d]Imidazole-7-Carboxylate

该化合物是一种主要用于高血压治疗的血管受体第二受体抗体,是一种在身体中转化成活性形式的抗药剂,Azilsartan,有选择性地阻塞二类血管1受体,导致血管变异和降血压.Azilsartan medoxomil 的化学配方反映了其复杂结构,包括一个双苯基和一种碳酸味.该化合物的特点是其高能和长效作用,使其对一次剂量有效.Azilsartan medoxomil 通常通过口服和强效注射,其致癌性受食物摄入等因素影响.常见副作用包括眩晕,疲劳和胃肠扰动.与其他抗血激素剂一样,在治疗期间必须监测肾功能和电解水平,使其对一次剂量有效.

英文名称(5-Methyl-2-Oxo-1,3-Dioxol-4-yl)Methyl 2-Ethoxy-1-((2'-(5-Oxo-4,5-Dihydro-1,2,4-Oxadiazol-3-yl)-[1,1'-Biphenyl]-4-yl)Methyl)-1H-Benzo[d]Imidazole-7-Carboxylate
中文名称阿齐沙坦奥美沙坦酯
IUPAC名称(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl 2-ethoxy-1-((2'-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylate
其它别名1-[[2'-(2,5-Dihydro-5-oxo-1,2,4-oxadiazol-3-yl)[1,1'-biphenyl]-4-yl]methyl]-2-ethoxy-1H-benzimidazole-7-carboxylic acid (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl ester; Azilsartan medoxomil
CAS编号863031-21-4
MFCD编号:MFCD19443688
FDA UNII编号:LL0G25K7I2
分子式:C30H24N4O8
分子量:568.54
产品CID: 1864188
同类组份化合物CAS863031-24-7 (potassium)863031-21-4 (free acid)
产品分类生物化工 → 抑制剂 → 内分泌及激素 → 肾素-血管紧张素-醛固酮系统拮抗剂

相似结构搜索
InChIKey: QJFSABGVXDWMIW-UHFFFAOYSA-N
QJFSABGVXDWMIW-UHFFFAOYSA-N…
计算化学: 氢键受体数10.0氢键供体数1.0可旋转键数10.0

物理性质

熔点160-161°C
沸点748.0±70.0 °C at 760 mmHg
闪点406.2±35.7 °C
密度1.5±0.1 g/cm3
pKa:6.99±0.20(预测)
PSA:155.59
LogP:5.73
折射率1.680
蒸汽压0.0±2.5 mmHg at 25°C
溶解性DMSO (Slightly), Methanol (Slightly, Heated, Sonicated)
外观形态白色至浅米色固体
储存条件冰箱
产品应用该化合物用于降低高血压的长效血管二型受体阻塞器(ARB) . 当AZILLSARTON MEDXOMIL进入肠胃道时,它会迅速转化为活性形式AZIRSARANT(A926900).

上下游产品

合成工艺路线路线简述

合成目标产物 Azilsartan Medoxomil 主要起始原料 4-(Hydroxymethyl)-5-Methyl-1,3-Dioxol-2-One And Azilsartan
80841-78-7 + 147403-03-0 = 863031-21-4
反应条件:1.1 Catalysts: 1,8-Diazabicyclo[5.4.0]Undec-7-Ene
标题:Related Substances Of Azilsartan Medoxomil: Synthesis And Characterization
作者:Sethi,Madhuresh K.; Et Al
参考文献:Pharma Chemica 日期:2015 卷标:7(1) 页码:20-28]

74124-79-1 + 1449029-77-9 = 863031-21-4
反应条件:1.1 Solvents: Ethyl Acetate; 25 - 30 °C; 16 H,40 - 45 °C
标题:Commercial Synthesis Of Azilsartan Kamedoxomil: An Angiotensin Ii Receptor Blocker
作者:Garaga,Srinivas; Et Al
参考文献:Organic Process Research & Development 日期:2015 卷标:19(4) 页码:514-519]

91526-18-0 + 147403-03-0 = 863031-21-4
反应条件:1.1 Reagents: Tosyl Chloride
标题:Study On The Synthetic Technology Of Azilsartan Medoxomil
作者:Jia,Jing-Yu; Et Al
参考文献:Huaxue Yanjiu Yu Yingyong 日期:2014 卷标:26(3) 页码:413-417]

863031-21-4 + 127-19-5 = 863031-21-4
反应条件:1.1 Solvents: Acetone,Water; 3 H,40 °C; 40 °C -> 25 °C; 1 H,25 °C
标题:Improved Process For Azilsartan Medoxomil: A New Angiotensin Receptor Blocker
作者:Radl,Stanislav; Et Al
参考文献:Organic Process Research & Development 日期:2013 卷标:17(1) 页码:77-86]

139481-44-0 = 863031-21-4 [标题:Reaction Conditions
标题:Synthesis And Characterization Of Impurities Of A Common And Advanced Intermediate Of Candesartan And Azilsartan Antihypertensive Drugs
作者:Sangwan,Sangeeta; Et Al
参考文献:International Research Journal Of Pure And Applied Chemistry 日期:2015 卷标:5(2) 页码:1-10

海关参考信息

2906210000-苄醇
2912110000-甲醛
2912210000-苯甲醛
2915110000-甲酸
💡 提示：海关信息按照顺序优先匹配，如需确认的海关信息，请参考相关资料。
详情请参考：📖 海关编码查询和海关进出口税则

专利信息

专利号:US-10005720-B2
优先权日:2013-04-05
标题:Compounds useful for the treatment of metabolic disorders and synthesis of the same
发明人：SEXTON JONATHAN Z; BRENMAN JAY E; MUSSO DAVID L
权利人:NORTH CAROLINA CENTRAL UNIV; UNIV NORTH CAROLINA CHAPEL HILL
摘要:The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.

专利号:US-10300471-B2
优先权日:2013-10-08
标题 :Ruthenium-catalyzed synthesis of biaryl compounds in water
发明人：KOOHANG ALI AIDEN; MEHTA ANITA
权利人:CHICAGO DISCOVERY SOLUTIONS LLC
摘要:Using a [RuCl 2 (arene)] 2 complex and a formate source, a directed ortho Câ€”H insertion and aryl-aryl coupling sequence in water provides biaryl compounds useful in the preparation of biologically active molecules and intermediates. Reactions may be conducted in the ambient atmosphere. Ruthenium catalysts prepared from [RuCl 2 (arene)] 2 and a formate source may be prepared in situ or isolated for later use.

专利号:US-2018370905-A1
优先权日:2013-04-05
标题:Compounds Useful for the Treatment of Metabolic Disorders and Synthesis of the Same

专利号:US-2016046560-A1
优先权日:2013-04-05
标题 :Compounds useful for the treatment of metabolic disorders and synthesis of the same

专利号:US-2016263565-A1
优先权日:2013-10-08
标题:Ruthenium-catalyzed synthesis of biaryl compounds in water

专利号:WO-2015054120-A1
优先权日:2013-10-08
标题 :Ruthenium-catalyzed synthesis of biaryl compounds in water

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