CAS: 247257-48-3; 2-(1-((2'-(2H-Tetrazol-5-yl)-[1,1'-Biphenyl]-4-yl)Methyl)-2-Butyl-4-Methyl-6-Oxo-1,6-Dihydropyrimidin-5-yl)-N,N-Dimethylethanethioamide

该化合物是一种主要用于治疗高血压的血管受体二型受体敌者;它属于被称为Sartans的药物类别,它通过阻塞血管二型的动作而发挥作用,这种激素导致血管血管收缩,从而降低血压;Fimasartan的特征是选择性抑制AT1受体,这助长了其抗血压效应;该物质通常通过口服施用,具有相对较长的半衰期,允许每天服一次药;就其化学结构而言,Fimasartan具有独特的分子框架,其中包括双联细胞细胞和碳盒酸组,有助于其药性;它一般是良好的,其副作用与该类的其他药物相似,包括头晕,疲劳和潜在的肾效应;与任何药物一样,它必须在医疗监督下使用Fimasartan,考虑到与其他药物和个人的健康状况可能发生相互作用.

结构式图片

上下游产品

2-n-butyl-5-dimethylamin°Carbonylmethyl-6-methyl-3-[[2'-(N-triphenylmethyltetrazol-5-yl)biphenyl-4-yl]methyl]pyrimidin-4(3H)-one

合成工艺路线路线简述

  • 合成目标产物 Fimasartan 主要起始原料 2-(2-Butyl-4-Methyl-6-Oxo-1-((2'-(1-Trityl-1H-Tetrazol-5-yl)-[1,1'-Biphenyl]-4-yl)Methyl)-1,6-Dihydropyrimidin-5-yl)-N,N-Dimethylethanethioamide
  • (文献来源)合成步骤主要原料 2-(2-Butyl-4-Methyl-6-Oxo-1-((2'-(1-Trityl-1H-Tetrazol-5-yl)-[1,1'-Biphenyl]-4-yl)Methyl)-1,6-Dihydropyrimidin-5-yl)-N,N-Dimethylethanethioamide
2-(1-((2'-(1氢-四唑-5-基)-[1,1'-联苯]-4-基)甲基)-2-丁基-4-甲基-6-羰基-1,6-二氢嘧啶-5-基)-N,N-二甲基乙酰胺置于劳森试剂体系中,用 甲苯 用作溶剂,化学反应 3.0H,以80%的收率获得非马沙坦
参考文献:一种非马沙坦的合成方法
标题:一种非马沙坦的合成方法
摘要:本发明公开了一种非马沙坦的合成方法,是在甲苯中化合物vi与化合物vii反应得到化合物v;化合物v与戊脒盐酸盐在碱金属氢氧化物存在下反应得到化合物iv;化合物iv在甲苯和dmf组成的混合溶剂中用氢化锂拔氢,然后与2‑氰基‑4'‑溴甲基联苯发生n‑烷基化反应得到化合物iii;化合物iii和叠氮化钠在氯化锌催化下在dmf中反应得到化合物ii;化合物ii与劳森试剂发生硫代酰胺化反应得到目标产物i.本发明工艺简单,操作简便,原料易得,经济高效,极大地降低了非马沙坦的生产成本,易于实现工业化生产.

海关参考信息

专利信息


专利号:US-10973847-B2
优先权日:2017-06-30
标题 :Core-to-surface polymerization for the synthesis of star polymers and uses thereof
发明人:JOHNSON JEREMIAH A; GOLDER MATTHEW R
权利人:MASSACHUSETTS INST TECHNOLOGY
摘要:Disclosed are methods, compositions, reagents, systems, and kits to prepare star polymers, as well as compositions and uses thereof. Various embodiments show that synthesis of these polymers contain low metal concentration to provide polymers for diverse biomedical applications including in vivo applications.

专利号:US-2024368164-A1
优先权日:2021-04-28
标 题 :Purine nucleosides, their intermediates, and methods of preparation thereof
发明人:RAVI RAMA SURESH; JACOBSON KENNETH A; POE RUSSELL BIRCH
权利人:ASTROCYLE PHARMACEUTICALS INC; US HEALTH
摘要:The present invention provides purine nucleoside analog compounds and methods of use thereof for treatment of certain injuries, disorders and conditions, for example brain injuries such as stroke or traumatic brain injuries. The present invention further provides methods of synthesizing such compounds, and intermediates useful in the synthesis of such compounds.

专利号:US-11485721-B2
优先权日:2017-11-21
标 题:Method for the metal-free preparation of a biaryl by a photosplicing reaction and their uses
发明人:KLOSS FLORIAN; NEUWIRTH TONI; HAENSCH VEIT; HERTWECK CHRISTIAN
权利人:LEIBNIZ INST FUER NATURSTOFF FORSCHUNG UND INFEKTIONSBIOLOGIE E V HANS KNOELL INST HKI; LEIBNIZ INST FUER NATURSTOFF FORSCHUNG UND INFEKTIONSBIOLOGIE E V HANS KNOELL INST
摘要:The present invention relates to a method for the metal-free preparation of a biaryl compound by a photosplicing reaction and its use in the preparation of chemical compounds, preferably of active ingredients e.g. in the fields of pharmaceuticals and agrochemicals. In particular, it refers to a method for the regiocontrolled preparation of a biaryl compound of formula (I): Ar—Ar′ by photochemically reacting a precursor compound of formula (II): Ar—L—Ar′ to form a biaryl compound of general formula: Ar—L—Ar′(II)→Ar—Ar′ (I) wherein Ar and Ar′, independently of each other, represent an unsubstituted or substituted C6-C20 aryl group or a heteroaryl group with 5-20 ring atoms selected from carbon, nitrogen, oxygen and sulfur, and L represents a group —X—Y—Z— as defined herein. The biaryl compounds are generally suitable as intermediates or key building blocks in a very broad spectrum of organic chemical syntheses and their respective utilities. Their use within the field of synthesis of active ingredients is an aspect of the invention, and their use in the preparation of pharmaceutically active ingredients is particularly preferred.

专利号:EP-3645600-A1
优先权日:2017-06-30
标题 :Core-to-surface polymerization for the synthesis of star polymers and uses thereof

专利号:US-2025049968-A1
优先权日:2022-04-21
标 题 :Therapeutic and imaging agents for targeting myocardial tissue
发明人:EEDA VENKATESWARARAO; AWASTHI VIBHUDUTTA
权利人:UNIV OKLAHOMA
摘要:Analogs and derivatives of omecamtiv mecarbil (OM), including an 18F-labeled analog, and methods of synthesis thereof. Cardiac myosin targeting vectors comprising a lipid anchoring/solubilizing moiety conjugated to a head made of OM or the OM analog or derivative. Liposomes comprising a cardiac-treating cargo molecule and the cardiac myosin targeting vector. Methods of treating a cardiac condition or disease in a subject by administering to the subject the cardiac-treating cargo molecule and the cardiac myosin targeting vector. Methods of synthesizing an 18F-labeled analog of OM.

专利号:CN-107973784-B
优先权日:2017-11-16
标题 :Synthesis method of fimasartan
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主要参考文献


1: Kim CK, Yang XL, Kim YJ, Choi IY, Jeong HG, Park HK, Kim D, Kim TJ, Jang H, Ko SB, Yoon BW. Effect of Long-Term Treatment with Fimasartan on Transient Focal Ischemia in Rat Brain. Biomed Res Int. 2015;2015:295925. doi: 10.1155/2015/295925. Epub 2015 Sep 13.
2: Ghim JL, Paik SH, Hasanuzzaman M, Chi YH, Choi HK, Kim DH, Shin JG. Absolute bioavailability and pharmacokinetics of the angiotensin II receptor antagonist fimasartan in healthy subjects. J Clin Pharmacol. 2015 Aug 13. doi: 10.1002/jcph.618. [Epub ahead of print] doi: 10.2147/DDDT.S82098. eCollection 2015.
4: Lee JY, Choi YJ, Oh SJ, Chi YH, Paik SH, Lee KH, Jung JK, Ryu CS, Kim KB, Kim DH, Yoon YR, Kim SK. Characterization of fimasartan metabolites in human liver microsomes and human plasma. Xenobiotica. 2015 Jun

合成参考文献


参考文献:10.1097/fjc.0b013e31822b9092
摘要:Shin KH, Kim TE, Kim SE, Lee MG, Song IS, Yoon SH, Cho JY, Jang IJ, Shin SG, Yu KS. The effect of the newly developed angiotensin receptor II antagonist fimasartan on the pharmacokinetics of atorvastatin in relation to OATP1B1 in healthy male volunteers. J Cardiovasc Pharmacol. 2011 Nov;58(5):492–9. doi: 10.1097/fjc.0b013e31822b9092.
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