CAS: 885-70-1; 5,11-Dihydropyrido[2,3-B][1,4]Benzodiazepin-6-One

该化合物是一种属于苯并二氮杂卓类化学品的杂交化合物,其特点是一个结合的双环结构,包括一个苯环和二氮苯并酯,有助于其独特的化学特性;其特点是含有氮的异丙环,可影响其生物活动和药理特性;该化合物通常在药用化学中表现出一系列潜在的应用,特别是在开发厌毒剂,镇静剂或抗凝解剂方面;其结构特征还可能允许与各种生物目标,包括...

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CAS号956-30-9 2-氨基-N-(2-氯吡啶-3... | CAS号84772-28-1 2,3,4,4a,5,11-h... | CAS号39620-04-7 3-氯-2-氨基吡啶 | CAS号87-25-2 2-氨基苯甲酸乙酯 | CAS号1028-86-0 2-氯-3-(2-硝基苯甲酰氨基)吡啶 | CAS号552-16-9 2-硝基苯甲酸 | CAS号610-14-0 2-硝基苯甲酰氯 | CAS号6298-19-7 2-氯-3-氨基吡啶 | CAS号134-20-3 邻氨基苯甲酸甲酯 | CAS号102394-31-0 11-((2-((二乙氨基)甲... | CAS号28797-48-0 5,11-二氢-11-氯乙酰基... | CAS号28797-61-7 哌仑西平 | CAS号88369-80-6 2-[(3-amino-1-o... | CAS号79276-54-3 6H-Pyrido(2,3-b... | CAS号84446-11-7 11-(2-imidazol-... | CAS号88369-79-3 2-[(3-amino-1-h...

合成工艺路线路线简述

  • 956-30-9 = 885-70-1 [标题:Reaction Conditions
    标题:New Synthesis Of 11-Acyl-5,11-Dihydro-6H-Pyrido[2,3-B][1,4]Benzodiazepin-6-Ones And Related Studies
    作者:Kovac,T.; Oklobdzija,M.; Comisso,G.; Decorte,E.; Fajdiga,T.; Et Al
    参考文献:Journal Of Heterocyclic Chemistry 日期:1983 卷标:20(5) 页码:1339-49]

    956-30-9 = 885-70-1 [标题:Reaction Conditions
    标题:Synthesis Of Pirenzepine - A Drug For Peptic Ulcer
    作者:Feng,Juncai; Wu,Meifang; Zhang,Lin; Sha,Jian; Chen,Weixing
    参考文献:Yiyao Gongye 日期:1984 卷标:(2) 页码:12-14]

    87-25-2 + 6298-19-7 = 885-70-1
    反应条件:1.1 Reagents: Potassium Tert-Butoxide Solvents: 1,4-Dioxane; 2 Min,Rt -> 60 °C; 10 Min,60 °C; 3 Min,60 °C -> 100 °C; 2.5 H,100 °C; 100 °C -> Rt1.2 Reagents: Monosodium Phosphate Solvents: Water; 30 Min,Rt
    标题:A New Synthetic Route To Compounds Of The Afdx-Type With Affinity To Muscarinic M2-Receptor
    作者:Holzgrabe,Ulrike; Heller,Eberhard
    参考文献:Tetrahedron 日期:2003 卷标:59(6) 页码:781-787]

    956-30-9 = 885-70-1
    反应条件:1.1 5 Min,210 °C
    标题:Fluorescent Pirenzepine Derivatives As Potential Bitopic Ligands Of The Human M1 Muscarinic Receptor
    作者:Tahtaoui,Chouaib; Parrot,Isabelle; Klotz,Philippe; Guillier,Fabrice; Galzi,Jean-Luc; Et Al
    参考文献:Journal Of Medicinal Chemistry 日期:2004 卷标:47(17) 页码:4300-4315]

    956-30-9 = 885-70-1 [标题:Reaction Conditions
    标题:Experimental Antiulcer Agents: N-Substituted 2-(4-Methyl-1-Piperazinyl)Acetamides As Pirenzepine Models And Some Related Compounds
    作者:Hulinska,Hana; Polivka,Zdenek; Jilek,Jiri; Sindelar,Karel; Holubek,Jiri; Et Al
    参考文献:Collection Of Czechoslovak Chemical Communications 日期:1988 卷标:53(8) 页码:1820-44]

    87-25-2 + 6298-19-7 = 885-70-1
    反应条件:1.1 Reagents: Potassium Tert-Butoxide Solvents: 1,2,4-Trichlorobenzene; Rt; Rt -> 85 °C; 4 H,85 °C; 14 H,85 °C -> 215 °C
    标题:Synthesis And Radiosynthesis Of N5-[18F]Fluoroethyl-Pirenzepine And Its Metabolite N5-[18F]Fluoroethyl-Ls 75
    作者:Riss,Patrick J.; Soskic,Vukic; Schrattenholz,Andre; Roesch,Frank
    参考文献:Journal Of Labelled Compounds And Radiopharmaceuticals 日期:2009 卷标:52(14) 页码:576-579]

    = 885-70-1
    反应条件:1.1 Catalysts: Pyridine
    标题:Novel Synthesis Of 5,11-Dihydro-6H-Pyrido[2,3-B][1,4]Benzodiazepin-6-Ones And Related Studies. Part I
    作者:Oklobdzija,M.; Comisso,G.; Decorte,E.; Fajdiga,T.; Gratton,G.; Et Al
    参考文献:Journal Of Heterocyclic Chemistry 日期:1983 卷标:20(5) 页码:1329-34
📜邻硝基苯甲酸置于氯化亚砜,铁粉,溶剂黄146,三乙胺,Potassium Iodide体系中,用 乙醇,二氯甲烷,甲苯 作为反应溶剂,化学反应 9.0H,反应生成 5,11-二氢-6H-吡啶并[2,3-B][1,4]苯并二氮杂-6-酮
参考文献:一种肠胃药盐酸哌仑西平重要中间体的简便合成工艺
标题:一种肠胃药盐酸哌仑西平重要中间体的简便合成工艺
摘要:本发明公开了一种肠胃药盐酸哌仑西平重要中间体的简便合成工艺,针对5,11‑二氢‑11‑氯乙酰基‑6H‑吡啶并[2.3‑b][1,4]苯并二氮卓‑6‑酮的合成,开发出了一条原料简单易得,操作简单的合成工艺,以邻硝基苯甲酸和2‑氯‑3‑氨基吡啶为主原料,五步合成目标化合物,成本低,收率高,纯度高,对最终药物有深远的现实意义.

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专利信息


专利号:US-4308206-A
优先权日:1980-03-17
标 题:Process for preparing derivatives of 5,11-dihydro-6h-pyrido[2,3-b][1,4]-benzodiazepin-6-one, and the final derivatives and synthesis intermediates obtained thereby
发明人：GERSZBERG SZEPSEL
权利人:MICROSULES ARGENTINA SA
摘要:This invention relates to a process for preparing derivatives of 5,11-dihydro-6H-pyrido[2,3-b][1,4]-benzodiazepin-6-one of general formula (I) ##STR1## in which R is hydrogen, halogen or methyl; n R 1 and R 2 are linear or branched C 2 -C 4 alkyl groups, which alternatively may be joined together to give a piperazine cycle which can be substituted in position 4 with a methyl, ethyl or benzyl group, n and their salts with organic and inorganic acids, characterised by comprising the following stages: n (a) reacting a compound of general formula (X), ##STR2## in which R has the meaning heretofore defined, with 2-cloro-3-amino-pyridine of formula (III) ##STR3## in the presence of polyphosphoric acid, to give an intermediate of general formula (II) ##STR4## (b) reacting said intermediate with a compound of general formula (XI) ##STR5## in which R 1 and R 2 have the meaning heretofore defined and R 3 is a hydroxyl or halogen, in an inert solvent at a maximum temperature equal to the solvent boiling point, to give said derivatives of general formula (I). n The invention also relates to the final compounds thus obtained, and the synthesis intermediates obtained during the course of said process. n The final products of formula (I) are of great interest in the pharmaceutical field.

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合成参考文献


摘要:Kleemann, A.; Engel, J.; Kutscher, B.; Reichert, D., Pharmaceutical Substances[Online], Thieme: Stuttgart, (2003).
摘要:Herr, R. J., Science of Synthesis, (2004) 17, 968.
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