CAS: 28797-61-7; 11-(2-(4-Methylpiperazin-1-yl)Acetyl)-5,11-Dihydro-6H-Benzo[e]Pyrido[3,2-B][1,4]Diazepin-6-One

该化合物是一种选择性的肌肉受体对立物,主要用于治疗胃溃疡和胃肠紊乱,其作用是抑制肌肉受体的乙酰胆碱,特别是M1亚型,减少胃酸分泌,促进胃肌肉保护.该化合物的特征是其M1受体与其他肌肉受体亚型相比具有相对较高的亲近性,它有助于其治疗效果,其副作用与更广泛的抗胆碱性活性活动有关,较少.Pirenzepine通常通过口服施用,具有适度的生物利用率.其药理学涉及肝脏新陈代谢,主要通过尿液排出.已知该物质的潜在副作用包括干口,视力模糊和内分泌,这是典型的抗胆碱剂.

结构式图片

上下游产品

1-methyl-piperazine 11-(chloroacetyl)-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one chloroacetyl chloride

合成工艺路线路线简述

    📜5,11-二氢-6H-吡啶并[2,3-B][1,4]苯并二氮杂-6-酮置于三乙胺体系中,用 1,4-二氧六环,苯 用作溶剂,化学反应 26.0H,反应生成哌仑西平
    参考文献:Hulinska,Hana; Polivka,Zdenek; Jilek,Jiri,Collection Of Czechoslovak Chemical Communications,1988,Vol. 53,# 8,P. 1820-1844
    标题:Hulinska,Hana; Polivka,Zdenek; Jilek,Jiri,Collection Of Czechoslovak Chemical Communications,1988,Vol. 53,# 8,P. 1820-1844

    海关参考信息

    专利信息


    专利号:US-2006167025-A1
    优先权日:2004-12-22
    标 题:Tricyclic amino alcohols, processes for synthesis of same and use of same as anti-inflammatory drugs
    发明人:BERGER MARKUS; SCHMEES NORBERT; SCHAECKE HEIKE; BAURLE STEFAN; REHWINKEL HARTMUT; MENGEL ANNE; KROLIKIEWICZ KONRAD; GROSSBACH DANJA; VOIGTLAENDER DAVID
    权利人:BERGER MARKUS; SCHMEES NORBERT; SCHAECKE HEIKE; BAURLE STEFAN; REHWINKEL HARTMUT; MENGEL ANNE; KROLIKIEWICZ KONRAD; GROSSBACH DANJA; VOIGTLAENDER DAVID
    摘要:The invention relates to tricyclic amino alcohols of general formula (I) n nmethod for synthesis of same and use of same as anti-inflammatory agents.

    专利号:US-2008280855-A1
    优先权日:2005-06-22
    标 题 :Process For the Production of Intermediates For the Preparation of Tricyclic Benzimidazoles
    发明人:CHIESA MARIA VITTORIA; PALMER ANDREAS; BUHR WILM; ZIMMERMANN PETER JAN; BREHM CHRISTOF; SIMON WOLFGANG-ALEXANDER; POSTIUS STEFAN; KROMER WOLFGANG; ZANOTTI-GEROSA ANTONIO
    权利人:NYCOMED GMBH
    摘要:The invention relates to a process for the synthesis of compounds of the formula 1-a and compounds of the formula 1-b. n n n n n n n n n n The compounds of the formula 1-a and the compounds of the formula 1-b, in which the substituents R1, R2, R3, and Ar have the meanings indicated in the description, are valuable intermediates for the preparation of pharmaceutically active compounds.

    专利号:EP-1639157-B1
    优先权日:2003-06-27
    标 题:Method of synthesising a crystalline material and material thus obtained
    发明人:PRIBAT DIDIER
    权利人:CENTRE NAT RECH SCIENT
    摘要:The invention provides a method of synthesizing a crystalline material in which seeds ( 6 ) are produced of a catalyst that is adapted to dissolve carbon on a substrate ( 2 ) of a first material; carbon nanotubes ( 6 ) are grown from the seeds ( 6 ); and a layer is produced of a second material comprising at least one monocrystalline region ( 12 ) orientated from a seed ( 6 ). The invention also provides the material obtained by said method. Application to the synthesis of polycrystalline silicon on a glass substrate.

    专利号:US-11612610-B2
    优先权日:2018-12-14
    标题:Mito-magnolol compounds and methods of synthesis and use thereof
    发明人:KALYANARAMAN BALARAMAN; ZIELONKA JACEK MICHAL; CHENG GANG; HARDY MICAEL JOËL; OUARI OLIVIER
    权利人:MEDICAL COLLEGE WISCONSIN INC; AIX MARSEILLE UNIV; MEDICAL COLLEGE OF WISCONSIN INC
    摘要:The present invention provides mito-magnolol compounds, pharmaceutical compositions thereof, and methods of using the mito-magnolol compounds in the treatment of cancer, especially anti-cancer therapy or kinase resistant cancers.

    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.

    专利号:US-6150129-A
    优先权日:1996-08-01
    标 题 :Antimicrobial determination of N-(aminoalkyl) and/or N-(Amidoalkyl) dinitrogen heterocyclic compositions
    发明人:COOK PHILLIP DAN; KAWASAKI ANDREW M; KUNG PEI PEI
    权利人:ISIS PHARMACEUTICALS INC
    摘要:Compositions are provided comprising novel di-nitrogen heterocycle compounds containing N-(aminoalkyl) and/or N-(amidoalkyl) groups. An additional situs of functionality is also provided. The compounds and compositions of the invention are useful as antibacterial and other pharmaceutical agents and as intermediates for preparation of other pharmaceutical agents. In addition, compounds of the present invention are useful as research reagents including employment as species for effecting combinatorial synthesis.

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    主要参考文献


    1: Del Tacca M, Danesi R, Blandizzi C, Bernardini MC. Un antimuscarinico selettivo: la pirenzepina. Rassegna delle sue proprietà farmacologiche e cliniche [A selective antimuscarinic agent: pirenzepine. Review of its pharmacologic and clinical properties]. Minerva Dietol Gastroenterol. 1989 Jul- Sep;35(3):175-89. Italian. 11(1):23397. doi: 10.1038/s41598-021-02732-y.
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    合成参考文献


    参考文献:10.1021/cb900276p
    摘要:Stewart GD, Sexton PM, Christopoulos A. Detection of Novel Functional Selectivity at M3 Muscarinic Acetylcholine Receptors Using a Saccharomyces cerevisiae Platform. ACS Chem. Biol. 2010 Feb 23;5(4):365–75. doi: 10.1021/cb900276p.
    参考文献:10.1152/japplphysiol.00779.2005
    摘要:Tobin G, Ryberg AT, Gentle S, Edwards AV. Distribution and function of muscarinic receptor subtypes in the ovine submandibular gland. J Appl Physiol (1985). 2006 Apr;100(4):1215–23. doi: 10.1152/japplphysiol.00779.2005.
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