CAS: 596-51-0; 3-(2-Cyclopentyl-2-Hydroxy-2-Phenylacetoxy)-1,1-Dimethylpyrrolidin-1-Ium Bromide

该化合物是属于抗胆碱酯酶制剂类的合成四硝基铵化合物,属于该类抗胆碱酯酶,主要用于临床环境,以减少手术过程中呼吸道的流露和分泌,以及管理诸如胃溃疡和过多出汗等条件. 催化器的特点是,它有能力竞争性地抑制肌肉受体的乙酰胆碱作用,导致腺分泌减少和肌肉放松.该物质通常通过口服或注射途径施用,而且与其他抗胆碱剂相比,其作用相对较长,已知其作用时间相对较长.

结构式图片

欧盟法规

ECHA物质C&L通报REACH预注册

上下游产品

methyl bromide 3-(2-cyclopentyl-2-hydroxy-2-phenylacetyloxy)-1-methylpyrrolidine 1-methyl-3-pyrrolidinol 2-cyclopentyl-2-hydroxy-2-phenylacetic acid3-[(cyclopentylhydroxyphenylacetyl)oxy]-1,1-dimethylpyrrolidinium iodide [(cyclopentyl-hydroxyphenylacetyl)oxy]-1,1-dimethylpyrrolidinium chloride [(cyclopentyl-hydroxyphenylacetyl)oxy]-1,1-dimethylpyrrolidinium chloride 3-[(cyclopentylhydroxyphenylacetyl)oxy]-1,1-dimethyl-pyrrolidinium benzoate

合成工艺路线路线简述

    Cyclopentylglyoxylsaeure置于4-二甲氨基吡啶,Magnesium,N,N'-二环己基碳二亚胺体系中,用 四氢呋喃,二氯甲烷,氯仿,乙腈 作为反应溶剂,化学反应 73.0H,反应生成 甘罗溴铵
    参考文献: Process For Synthesis Of Glycopyrronium Bromide[fr] Procédé De Synthèse De Bromure De Glycopyrronium
    标题: Process For Synthesis Of Glycopyrronium Bromide[fr] Procédé De Synthèse De Bromure De Glycopyrronium
    摘要:本文提供了一种制备溴化甘可维铵的方法,包括将n-甲基吡咯烷-3-醇与式i或式ii化合物反应,随后进行额外的步骤.

    海关参考信息

    专利信息


    专利号:US-2025206743-A1
    优先权日:2022-03-25
    标 题:Tyk2 inhibitor synthesis and intermediates thereof
    发明人:MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG
    权利人:TAKEDA PHARMACEUTICALS CO
    摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.

    专利号:US-2022389172-A1
    优先权日:2021-06-04
    标 题:Synthesis of oligosaccharides as prebiotics from simple sugars and polysaccharides in concentrated acids
    发明人:PAN XUEJUN; ZENG MEIJUN; LI NING
    权利人:WISCONSIN ALUMNI RES FOUND
    摘要:Provided herein are methods for preparing a product including predominantly prebiotic oligosaccharides by non-enzymatic methods of glycosylation of monosaccharides, disaccharides, and/or polysaccharides. The methods may include mixing one or more types of monosaccharides, disaccharides, and/or polysaccharides with an effective amount of a dehydrating acid at a temperature sufficient to form a product including predominantly prebiotic oligosaccharides.

    专利号:US-3691198-A
    优先权日:1970-12-21
    标题 :Synthesis of 1-substituted-3-halopyrrolidines
    发明人:BROWN BERNARD BEAN; RUOPP DONALD CARL
    权利人:CPC INTERNATIONAL INC
    摘要:A method of preparing 1-substituted-3-halopyrrolidines, particularly a method of preparing said pyrrolidines by reacting a 1-substituted- Delta 3-pyrroline with a concentrated hydrogen halide aqueous solution at a temperature greater than 100*C. In a preferred embodiment, a supersaturated hydrobromic acid solution is utilized, i.e., one containing about 60 percent hydrogen bromide. The 1-substituted- Delta 3-pyrroline reactant is preferably made by reaction of a cis-1,4-dihalobutene-2 with a primary amine whereupon cyclization takes place. Said 1substituted-3-halopyrrolidines are intermediates useful in making anti-cholinergics and like materials.

    专利号:US-9757463-B2
    优先权日:2012-06-15
    标题 :Linear polyester and semi-linear glycidol polymer systems: formulation and synthesis of novel monomers and macromolecular structures
    发明人:HARTH EVA M; BEEZER DAIN B; LI GUANGZHAO; SPEARS BENJAMIN R; STEVENS DAVID M
    权利人:UNIV VANDERBILT
    摘要:Disclosed herein are glycidol-based polymers, nanoparticles, and methods related thereto useful for drug delivery. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

    专利号:WO-2018154597-A1
    优先权日:2017-02-22
    标题:Process for synthesis of glycopyrronium bromide
    发明人:REDDY G NITHUN; REDDY G SAMHITHA; REDDY G MADAALASA; RAMANI M; REDDY G PRATAP
    权利人:GBR LABORATORIES PVT LTD; RACHANA PHARMA TECH
    摘要:Provided herein are processes for preparation of glycopyrronium bromide comprising reaction of N-methylpyrrolidin-3-ol with compounds of Formula I or Formula II followed by additional steps.

    专利号:US-6030613-A
    优先权日:1995-01-17
    标题:Receptor specific transepithelial transport of therapeutics
    发明人:BLUMBERG RICHARD S; SIMISTER NEIL E; LENCER WAYNE I
    权利人:BRIGHAM & WOMENS HOSPITAL; UNIV BRANDEIS
    摘要:The present invention relates in general to methods and products for initiating an immune response against an antigen, and in particular relates to transepithelial delivery of antigens to provoke tolerance and immunity. The present invention further relates to methods and products for the transepithelial delivery of therapeutics. In particular, the invention relates to methods and compositions for the delivery of therapeutics conjugated to a FcRn binding partner to intestinal epithelium, mucosal epithelium and epithelium of the lung. The present invention further relates to the synthesis, preparation and use of the FcRn binding partner conjugates as, or in, pharmaceutical compositions for oral systemic delivery of drugs and vaccines.
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    主要参考文献


    1: Williams J, Cain N. Case report of successful treatment of pallid breath-holding spells with glycopyrrolate. Pediatrics. 2015 May;135(5):e1308-11. doi: 10.1542/peds.2014-2456. Epub 2015 Apr 13. doi: 10.1111/bcp.12517.
    3: D'Sa DJ, Lechuga-Ballesteros D, Chan HK. Isothermal microcalorimetry of pressurized systems II: effect of excipient and water ingress on formulation stability of amorphous glycopyrrolate. Pharm Res. 2015 Feb;32(2):714-22. doi: 10.1007/s11095-014-1499-8. Epub 2014 Sep 6. doi: 10.1111/jdv.12518. Epub 2014 Jun 9. doi: 10.1002/elps.201400170. Epub 2014 Oct 2. doi: 10.2146/ajhp130636. Erratum in: Am J Health Syst Pharm. 2014 Sep 15;71(18):1532. doi: 10.1111/aas.12452. Epub 2015 Jan 5. doi: 10.1016/j.jclinane.2013.05.007. Epub 2013 Sep 2. doi: 10.1111/evj.12032. Epub 2013 Mar 5. doi: 10.1001/jamadermatol.2014.4578. doi: 10.1111/pde.12236. Epub 2013 Nov 25. doi: 10.1111/jvp.12074. Epub 2013 Jul 31. doi: 10.1007/s12630-013-0064-y. Epub 2013 Dec 18. doi: 10.1007/s00540-015-2064-2. Epub 2015 Aug 9. doi: 10.1111/pde.12127. Epub 2013 Mar 28. doi: 10.1016/j.ijoa.2013.03.008. Epub 2013 May 18. doi: 10.1097/JCP.0000000000000102. doi: 10.1111/jvp.12085. Epub 2013 Dec 11. doi: 10.1164/rccm.201505-1048OC.

    合成参考文献


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    参考文献:10.1007/s00540-011-1190-8
    摘要:El Tahan MR. Effects of aminophylline on cognitive recovery after sevoflurane anesthesia. J Anesth. 2011 Oct;25(5):648–56. doi: 10.1007/s00540-011-1190-8.
    参考文献:10.1007/s12098-011-0524-8
    摘要:Grover S, Jindal A, Bansal A, Singhi SC. Acute bronchial asthma. Indian J Pediatr. 2011 Nov;78(11):1388–95. doi: 10.1007/s12098-011-0524-8.
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