CAS: 145733-36-4; 8-((2'-(1H-Tetrazol-5-yl)-[1,1'-Biphenyl]-4-yl)Methyl)-2,4-Dimethyl-5,6-Dihydropyrido[2,3-D]Pyrimidin-7(8H)-One

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抗体抗体,属于被称为Sartans的药物类别,它通过阻塞血管二型的动作起作用,这种激素抑制血管二型,抑制血管血管,增加血压.Tasosartan的化学配方反映了其复杂结构,包括双苯细胞和碳酸化合物,有助于其药理活动.它通常通过口服方式进行,以相对长的半衰期为人所知,允许每天服用一次.Tasosartan在肝脏中表现出良好的生物利用率,并经过新陈代谢,其代谢作用是其抗体性效应.常见副作用可能包括眩晕,疲劳和胃肠扰,尽管一般情况下情况良好.同其类别中的其他药物一样,Tasosartan在妊娠期间也以相对长的半衰期而闻名,允许使用一次.

结构式图片

上下游产品

5,8-Dihydro-2,4-Dimethyl-8-<(2'-(2-Tert-Butyl-2H-Tetrazol-5-yl)<1,1'-Biphenyl>-4-yl)Methyl>Pyrido<2,3-D>Pyrimidin-7(6H)-One 153042-17-2
2,4-Dimethyl-5,6,8-Trihydro-8-[[2'-(1-Tert-Butyl-1H-Tetrazol-5-yl)[1,1-Biphenyl]-4-Yl]Methyl]-7H-Pyrido[2,3-D]Pyrimidin-7-One 149049-80-9
8-[(4-溴苯基)甲基]-5,8-二氢-2,4-二甲基吡啶并[2,3-D]嘧啶-7(6H)-酮 2,4-Dimethyl-5,6,8-Trihydro-8-[(4-Bromophenyl)Methyl]-7H-Pyrido[2,3-D]Pyrimidin-7-One 145733-62-6

合成工艺路线路线简述

  • 合成目标产物 Tasosartan 主要起始原料 Ethanamine, N-[(3,5-Dichlorophenyl)Methylene]-2,2-Diethoxy-
  • (文献来源)合成步骤主要原料 Ethanamine, N-[(3,5-Dichlorophenyl)Methylene]-2,2-Diethoxy-
5,8-Dihydro-2,4-Dimethyl-8-<(2'-(2-Tert-Butyl-2H-Tetrazol-5-yl)<1,1'-Biphenyl>-4-yl)Methyl>Pyrido<2,3-D>Pyrimidin-7(6H)-One 以73的收率获得他索沙坦
参考文献:Substituted Pyrrolopyrimidines,Azepinopyrimidines And Pyridopyrimidines
标题:Substituted Pyrrolopyrimidines,Azepinopyrimidines And Pyridopyrimidines
摘要:本发明涉及一般式i的吡咯烷,吡啶,氮杂环庚烷和氮杂环吡咯嘧啶,其中r.Sup.1,R.Sup.2,R.Sup.3和r.Sup.4分别是h,含有1至6个碳原子的低碳基或含有1至6个碳原子的全氟碳基;R.Sup.5是h或当n为1时,R.Sup.5与r.Sup.3一起构成双键;N为0至1;P为0至2;M为0至3;Ar.Sup.1为##str2##其中w为h,含有1至6个碳原子的低碳基,卤素,羟基或含有1至6个碳原子的低烷氧基;Ar.Sup.2为##str3##其中x为##str4##其中r.Sup.6为h,叔丁基,三正丁基锡或三苯甲基;以及其药学上可接受的盐,由于其拮抗血管紧张素ii的能力,可用于治疗高血压,充血性心力衰竭和再狭窄.这些化合物也可用于降低血浆中的脂质水平,因此可用于治疗高脂血症和高胆固醇血症.还公开了生产该化合物的过程和含有该化合物的制药组合物.

海关参考信息

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-6271375-B1
优先权日:1997-06-30
标 题 :Ortho-metalation process for the synthesis of 2-substituted-1-(tetrazol-5-yl)benzenes
发明人:VILLA MARCO; ALLEGRINI PIETRO; ARRIGHI KATIUSCIA; PAIOCCHI MAURIZIO
权利人:ZAMBON SPA
摘要:A process of direct metalation of phenyltetrazoles useful for preparing compounds of formula (II) intermediates for the synthesis of angiotensin II antagonists is described.

专利号:US-8431712-B2
优先权日:2004-02-09
标 题 :Methods for the synthesis of pyridoxamine
发明人:KHALIFAH RAJA G; KEILITZ ROLAND; KOELLNER CHRISTOPH; DEGENHARDT THORSTEN; BRAND STEPHEN ROBERT
权利人:KHALIFAH RAJA G; KEILITZ ROLAND; KOELLNER CHRISTOPH; DEGENHARDT THORSTEN; BRAND STEPHEN ROBERT; NEPHROGENEX INC
摘要:The invention provides non-oxidative methods for the large scale manufacture of pyridoxamine (I) (4-aminomethyl-3-hydroxy-5-hydroxymethyl-2-methylpyridine): n nand salts thereof.n nThe invention also provides intermediate compounds for the synthesis of pyridoxamine, as well as compositions and methods for the treatment and/or prevention of conditions associated with the formation of post-Amadori advanced glycation end-products.

专利号:US-2008287407-A1
优先权日:2003-12-10
标题 :Nitric Oxide Releasing Pyruvate Compounds, Compositions and Methods of Use
发明人:GARVEY DAVID S; FANG XINQIN; KHANAPURE SUBHASH P; RANATUNGA RAMANI R; WEY SHIOW-JYI
权利人:NITROMED INC
摘要:The invention describes novel nitrosated and/or nitrosylated pyruvate compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated pyruvate compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one pyruvate compound and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one pyruvate compound, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating diseases resulting from oxidative stress, diabetes, reperfusion injury following ischemia, preservation of tissues, organs, organ parts and/or limbs.

专利号:US-3888844-A
优先权日:1971-09-10
标 题:Halogenated esters of phosphorus-containing acids (ii)
发明人:D ALELIO GAETANO F
权利人:ALELIO GAETANO F D
摘要:This invention deals with new phosphorus containing polymeric esters having pendent groups therein of the formula OBTAINED BY THE REACTION OF A POLYMER HAVING AT LEAST 2 AND PREFERABLY AT LEAST 4 HYDROXY GROUPS THEREIN WITH A PHOSPHORUSHALOGEN COMPOUND OF THE FORMULA XP(O) (ORCX CXR'')2 wherein: R represents a divalent hydrocarbon radical containing 1-20 carbon atoms; R'' represents X, hydrogen or R''''; R'''' represents a monovalent hydrocarbon radical containing 1-20 carbon atoms; and X represents chlorine or bromine. Somewhat related polymers are also disclosed as derived by the reaction of WHEREIN Q'' is an organic moiety, n'' has a value of at least one, n'''' is one or two, R'''''' represents hydrogen or a monovalent hydrocarbon group of 1-20 carbon atoms, and the other symbols have the same meaning as defined above. Also disclosed are the reaction products of the phosphite compound HOP(ORCX CXR'')2 with an aldehyde and an organic nitrogen compound having one or two hydrogen atoms on the nitrogen, or with a compound having an ethylenic group therein. These new ester polymers and compounds are useful particularly as fire retardants, agricultural chemicals, fuel additives, plasticizers, monomers and intermediates for the synthesis of other useful derivatives.

专利号:US-2025223262-A1
优先权日:2022-03-31
标 题 :Synthesis of morphinans with reduced herg activity and mop binding
发明人:LAMMERT ECKHARD; SCHOLZ OKKA; OTTER SILKE; HEREBIAN DIRAN; HOFFMANN TORSTEN; SANZ MIGUEL ANGEL; KRAMP LAURENZ; LEVY LAURA MARIANA; HRISTEVA STANIMIRA
权利人:HEINRICH HEINE UNIV DUESSELDORF; DEUTSCHE DIABETES FORSCHUNGSGESELLSCHAFT E V; TAROS CHEMICALS GMBH & CO KG
摘要:The invention relates to morphinan-derivatives, processes for their preparation, medicaments containing them and the use of these morphinan-derivatives for the preparation of medicaments.
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主要参考文献


1: Zuo H, Li T, Zhang D, Ma J, Zhang Z, Ou Y, Lian X, Yin J, Li Q, Zhao X. Enhancing Chromatographic Performance of Immobilized Angiotensin II Type 1 Receptor by Strain-Promoted Alkyne Azide Cycloaddition through Genetically Encoded Unnatural Amino Acid. Anal Chem. 2022 Nov 15;94(45):15711-15719. doi: 10.1021/acs.analchem.2c03130. Epub 2022 Nov 1. 40(5):2099-2112. doi: 10.1080/07391102.2020.1835721. Epub 2020 Oct 25.
3: Mujwar S, Deshmukh R, Harwansh RK, Gupta JK, Gour A. Drug Repurposing Approach for Developing Novel Therapy Against Mupirocin-Resistant Staphylococcus aureus. Assay Drug Dev Technol. 2019 Oct;17(7):298-309. doi: 10.1089/adt.2019.944. 2(3):314-5. doi: 10.1016/j.preghy.2012.04.249. Epub 2012 Jun 13. 12(15):1967-71. doi: 10.1016/s0960-894x(02)00303-7. (3):5-10. doi: 10.1080/08037050152518302. 295(2):649-54. 14(4):447-9. doi: 10.1023/a:1007876519124. 57(13):1231-41. doi: 10.1093/ajhp/57.13.1231. Erratum in: Am J Health Syst Pharm 2000 Nov 15;57(22):2036. Erratum in: Am J Health Syst Pharm 2001 May 15;58(10):864. 40(3):231-41. doi: 10.1177/00912700022008892. 384(1):81-9. doi: 10.1016/s0014-2999(99)00662-7. 15 Suppl F:26F-8F. 22(2):147-53. doi: 10.1291/hypres.22.147. 16(12 Pt 2):2085-9. doi: 10.1097/00004872-199816121-00034. 137(1):118-25. doi: 10.1016/s0002-8703(99)70467-9. 41(22):4251-60. doi: 10.1021/jm970690q. 11(4 Pt 1):454-61. doi: 10.1016/s0895-7061(97)00487-1. 10(12 Pt 2):311S-317S. doi: 10.1016/s0895-7061(97)00391-9. 37(4):542-50. doi: 10.1021/jm00030a013.

合成参考文献


参考文献:10.2165/00003088-199732010-00001
摘要:Csajka C, Buclin T, Brunner HR, Biollaz J. Pharmacokinetic-pharmacodynamic profile of angiotensin II receptor antagonists. Clin Pharmacokinet. 1997 Jan;32(1):1–29. doi: 10.2165/00003088-199732010-00001.
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