CAS: 81403-80-7; Alfuzosin

该化合物是一种主要用于治疗男性的良性先发性高血压(BPH)的药物,作为阿尔法-1肾上腺对抗剂,其行动机制包括放松前列腺和膀胱颈部的肌肉,这有助于改善尿流,减少与BPH有关的症状.从化学角度讲,Alfuzosin 具有结构特征,包括一种五氯硝基,有助于其药理特性.它通常通过口服,具有相对较长的半衰期,允许每天服用一次.该物质以选择使用甲型-1A 肾上腺受体为名,主要在前列腺部,最大限度地减少心血管的副作用,通常与非选择性甲型阻塞体有关.Alfusin 通常受到很好的调适,但潜在的副作用可能包括眩晕,疲劳和减肥.与任何药物一样,病人必须咨询保健专业人员,以便适当使用和讨论与其他药物的任何潜在互动.

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CAS号81403-67-0 N-(3-甲胺基丙基)四氢呋喃... | CAS号23680-84-4 4-氨基-2-氯-6, 7-二氧基喹唑啉 | CAS号16874-33-2 2-四氢呋喃甲酸 | CAS号76362-29-3 N1-methyl-N1-(4... | CAS号81403-68-1 盐酸阿夫唑嗪 | CAS号81403-69-2 N-(4-氨基-6,7-二甲氧... | CAS号1005197-73-8 1-(tetrahydrofu... | CAS号1100050-87-0 (R,S)-N-[3-[(4-... | CAS号52449-98-6 四氢呋喃-2-甲酰氯 | CAS号81403-68-1 盐酸阿夫唑嗪

合成工艺路线路线简述

  • 合成目标产物 Alfuzosin 主要起始原料 Tetrahydrofuran-2-Carboxylicacid(3-Methylamino-Propyl)-Amide And 2-Chloro-4-Amino-6,7-Dimethoxyquinazoline
  • (文献来源)合成步骤主要原料 Tetrahydrofuran-2-Carboxylicacid(3-Methylamino-Propyl)-Amide 和 2-Chloro-4-Amino-6,7-Dimethoxyquinazoline
盐酸阿夫唑嗪置于sodium Hydroxide体系中,用 二氯甲烷,水 作为反应溶剂,化学反应 0.25H,反应生成 阿夫唑嗪
参考文献: Crystalline Alfuzosin Base[fr] Base D'Alfuzosine Cristalline
标题: Crystalline Alfuzosin Base[fr] Base D'Alfuzosine Cristalline
摘要:本发明涉及晶体阿福唑辛基础物及其制备过程.例如,将阿福唑辛基础物(HPLC纯度:97%)加入甲醇中并加热至沸腾,形成清澈的溶液,然后将溶液冷却至25°-30oc并在相同温度下搅拌12小时,得到的溶液冷却至10°-15oc并搅拌2小时,然后过滤得到固体,用甲醇洗涤并在50°-60oc下干燥4小时,得到纯度为99.95%的阿福唑辛基础物.

海关参考信息

专利信息


专利号:US-10925977-B2
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

专利号:US-9765027-B2
优先权日:2014-08-22
标题 :Substituted 1-arylethyl-4-acylaminopiperidine derivatives as opioid/alpha-adrenoreceptor modulators and method of their preparation
发明人:VARDANYAN RUBEN S; HRUBY VICTOR J
权利人:THE ARIZONA BOARD OF REGENTS ON BEHALF OF THE UNIV OF ARIZAONA; UNIV ARIZONA
摘要:The invention provides compounds that bind with high affinities to the μ-, δ- and κ-opioid receptors and α 2 -adrenoreceptor. In addition to providing these compounds with novel pharmacological binding properties, the invention also describes detailed novel methods for the preparation of representative compounds and a scheme for the synthesis of related compounds that bind to the opioid receptors and/or α 2 -adrenoreceptor.

专利号:US-6469065-B1
优先权日:1996-02-02
标 题:Nitrosated and nitrosylated α-adrenergic receptor antagonist, compositions and methods of use
发明人:GARVEY DAVID S; SCHROEDER JOSEPH D; DE TEJADA INIGO SAENEZ; GASTON RICKY D; SHELEKHIN TATIANA E; WANG TIANSHENG
权利人:NITROMED INC
摘要:The present invention describes novel nitrosated and/or nitrosylated α-adrenergic receptor antagonists, and novel compositions containing at least one nitrosated and/or nitrosylated α-adrenergic receptor antagonist, and, optionally, one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or are a substrate for nitric oxide synthase, and/or one or more vasoactive agents. The present invention also provides novel compositions containing at least one α-adrenergic receptor antagonist, and one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents. The present invention also provides methods for treating or preventing sexual dysfunctions in males and females, for enhancing sexual responses in males and females, and for treating or preventing benign prostatic hyperplasia, hypertension, congestive heart failure, variant (Printzmetal) angina, glaucoma, neurodegenerative disorders, vasospastic diseases, cognitive disorders, urge incontinence, or overactive bladder, and for reversing the state of anesthesia.

专利号:WO-2009001369-A1
优先权日:2007-06-22
标 题 :An improved process for the preparation of alfuzosin hydrochloride
发明人:DEO KESHAV; DESAI SANJAY; RATHOD DHIRAJ MOHANSINH; PARIKH CHIRAG CHANDRAKANT; PATEL RIPALKUMAR KANTIBHAI
权利人:ALEMBIC LTD; DEO KESHAV; DESAI SANJAY; RATHOD DHIRAJ MOHANSINH; PARIKH CHIRAG CHANDRAKANT; PATEL RIPALKUMAR KANTIBHAI
摘要:The present invention relates to an improved process for the preparation of Alfuzosin hydrochloride of formula (I) comprising a step of reacting compound of formula (IV) with compound of formula (V) in presence of aprotic solvent to obtain compound of formula (III) which is a useful intermediate for synthesis of Alfuzosin hydrochloride of formula (I).

专利号:US-RE41998-E
优先权日:1990-02-26
标题 :Compositions and methods of treatment of sympathetically maintained pain
发明人:CAMPBELL JAMES N
权利人:ARCLON THERAPEUTICS INC
摘要:Sympathetically maintained pain is treated topically by administering to the site where sympathetically maintained pain is present an α-1-adrenergic antagonist, α-2-adrenergic agonist, or other drug that depletes or blocks synthesis of sympathetic norepinephrine, known collectively as sympatholytic agents. Chemical formulas for several sympatholytic agents are given.

专利号:WO-2008084493-A3
优先权日:2007-01-09
标 题 :A novel process for the preparation of 2-halo-4-aminoquinazolines
发明人:BHOBE AJIT MADHUKAR; DAMLE SUBHASH VISHWANATH; ADHVARYU RUSHI DRUPADBHAI
权利人:UNICHEM LAB LTD; BHOBE AJIT MADHUKAR; DAMLE SUBHASH VISHWANATH; ADHVARYU RUSHI DRUPADBHAI
摘要:2-Halo-4-aminoquinazolines are produced by a one-step process involving intramolecular cyclization of appropriately substituted formamide derivatives in the presence of phosphorous oxyhalides. Exemplary of the process is the intramolecular cyclization of 3,4-dimethoxy-6-cyanoaniline-1-yl formamide in the presence of phosphorous oxychloride to 2-chloro-4-amino-6,7-dimethoxyquinazoline. These chemical compounds are utilized as intermediates in the preparation of some of the important antihypertensive agents e.g. 2-chloro-4-amino-6,7-dimethoxyquinazolines is used for the synthesis of alfuzosin hydrochloride.
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合成参考文献


参考文献:10.2147/cia.s13803
摘要:Yoshida M, Kudoh J, Homma Y, Kawabe K. Safety and efficacy of silodosin for the treatment of benign prostatic hyperplasia. Clin Interv Aging. 2011;6():161–72.
参考文献:10.2147/tcrm.s13883
摘要:Masumori N. Naftopidil for the treatment of urinary symptoms in patients with benign prostatic hyperplasia. Ther Clin Risk Manag. 2011;7():227–38.
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