CAS: 50679-08-8; 1-(4-(Tert-Butyl)Phenyl)-4-(4-(Hydroxydiphenylmethyl)Piperidin-1-yl)Butan-1-Ol

该化合物是一种抗脊髓灰质炎,主要用于治疗干热和蜂窝等过敏条件;它属于第二代抗脊髓灰质炎类别,旨在与第一代抗脊髓灰质炎相比,最大限度地减少镇静剂.Terfenadine是H1肝胺受体的选择性敌物,有效阻止了过敏反应的化合物 ----肝胺 ----的动作;该物质的特点是水溶性相对较低,其亲血性使其很容易跨过细胞膜;然而,乙胺与严重的心脏副作用有关,特别是当它与某些抑制其代谢的药物一起服用时,导致潜在的威胁生命的异性.由于这些安全考虑,乙胺被从许多国家的市场上撤出,其化学结构包括一种三苯基乙醇的微生物,有助于其药用特性.因此,三氯丁胺不再被广泛使用,并且自此以来,已经开发出更安全的替代品用于各种治疗.

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

CAS号863029-85-0 1-(4-(tert-buty... | CAS号201230-82-2 carbon monoxide | CAS号115-46-8 二苯基(4-哌啶基)甲醇 | CAS号1025942-33-9 O-trimethylsily... | CAS号43076-30-8 特非那酮 | CAS号43076-61-5 4'-叔丁基-4-氯丁酰苯 | CAS号83799-24-0 非索芬那定 | CAS号43076-30-8 特非那酮

合成工艺路线路线简述

  • 合成目标产物 Terfenadine 主要起始原料 4'-Tert-Butyl-4-[4-(Hydroxybenzhydryl)Piperidino]Butyrophenone
  • (文献来源)合成步骤主要原料 4'-Tert-Butyl-4-[4-(Hydroxybenzhydryl)Piperidino]Butyrophenone
O-Trimethylsilyl Terfenadine置于苄基三甲基氟化铵体系中,用 四氢呋喃 作为反应溶剂,化学反应 72.0H,反应生成 特非那定
参考文献: Hydroaminomethylation Of Olefins[fr] Hydroaminomethylation D'Olefines
标题: Hydroaminomethylation Of Olefins[fr] Hydroaminomethylation D'Olefines

海关参考信息

专利信息


专利号:US-6803468-B2
优先权日:2000-08-29
标 题 :Process for the synthesis of n-(5-methylnicontinoyl)-4 hydroxypiperidine, a key intermediate of rupatadine
发明人:KUMAR YATENDRA; PRASAD MOHAN; SINGH SHAILENDRA KUMAR
权利人:RANBAXY LAB LTD
摘要:The present invention relates to an improved and industrially advantageous process for the preparation of N-(5-methylnicotinoyl)-4-hydroxypiperidine of Formula I, as shown in the accompanied drawings. This compound is a key intermediate for the synthesis of rupatadine, a potent dual antagonist of histamine and platelet-activating factor (PAF).

专利号:US-11311505-B2
优先权日:2017-02-24
标 题:Synergistic compositions to stimulate the synthesis of human lung and sinus surfactants to decrease coughing, increase FEV-1/FVC ratios, decrease lung fibrosis, by increasing apoptosis of myofibroblasts
发明人:MARTIN ALAIN
权利人:MARTIN ALAIN; CELLULAR SCIENCES INC
摘要:Methods for the treatment of patients with both Chronic Obstructive Pulmonary Disease (COPD) and pulmonary fibrosis, and of patients with idiopathic pulmonary fibrosis without COPD, by stimulating the synthesis of human and animal patient lung and sinus surfactants to increase lung functions, inhibiting fibrosis and reducing coughing and nasal erythema, include the following steps: A) analyzing and diagnosing a patient with a lung ailment selected from the group consisting of i) both COPD and pulmonary fibrosis; and ii) idiopathic pulmonary fibrosis without COPD; and, B) treating the patient to raise the patient's lung functions including FEV1/FVC ratio by contacting mammalian cells with a [therapeutically effective amount of a treatment] composition that includes: a) a pyruvate salt; b) a phosphate; c) a salt of calcium; and d) a salt of magnesium, in an aqueous carrier, containing no more than 2.2 grams of said pyruvate salt per liter.

专利号:US-5714127-A
优先权日:1992-10-08
标题 :System for multiple simultaneous synthesis
发明人:DEWITT SHEILA H H; KIELY JOHN S; PAVIA MICHAEL R; SCHROEDER MEL C; STANKOVIC CHARLES J
权利人:WARNER LAMBERT CO
摘要:A system for the multiple, simultaneous synthesis of compounds preferably uses a reaction apparatus comprising a reservoir rack having a plurality of reaction wells, a plurality of reaction tubes, usually gas dispersion tubes, having filters on their lower ends, a holder block, having a plurality of apertures, and a manifold, which has ports to allow introduction/maintenance of a controlled environment. The manifold top wall has a plurality of apertures in axial alignment with the reaction tubes and a gasket which allows penetration by a needle in order to dispense and aspirate materials from the reaction tubes. Sealing members, such as gaskets, are placed between the holder block, manifold and reservoir rack and the components are releasably fastened together. A robotic sample processor is used to automate the synthesis process using the reaction apparatus.

专利号:US-9982005-B2
优先权日:2013-04-04
标 题 :Macrolides and methods of their preparation and use
发明人:MYERS ANDREW G; SEIPLE IAN BASS; ZHANG ZIYANG
权利人:HARVARD COLLEGE
摘要:Provided herein are methods of preparing macrolides by the coupling of an eastern and western half, followed by macrocyclization, to provide macrolides, including both known and novel macrolides. Intermediates in the synthesis of macrolides including the eastern and western halves are also provided. Pharmaceutical compositions and methods of treating infectious diseases and inflammatory conditions using the inventive macrolides are also provided. A general diastereoselective aldol methodology used in the synthesis of the western half is further provided.

专利号:US-5702672-A
优先权日:1992-10-08
标 题 :Apparatus and method for multiple simultaneous synthesis
发明人:DEWITT SHEILA H H; KELL MICHAEL; PAVIA MICHAEL R; KIELY JOHN S; SCHROEDER MEL C; STANKOVIC CHARLES J; WARE STEVEN
权利人:WARNER LAMBERT CO
摘要:An apparatus for multiple, simultaneous synthesis of compounds which consists of: a reservoir block having a plurality of wells; a plurality of reaction tubes, usually gas dispersion tubes, having filters on their lower ends; a holder block, having a plurality of apertures; and a manifold, which may have ports to allow introduction/maintenance of a controlled environment. The manifold top wall has apertures and a detachable plate with identical apertures. The apparatus is constructed from materials which will accommodate heating, cooling, agitation, or corrosive reagents. Gaskets are placed between the components. Rods or clamps are provided for fastening the components together. Apparatus operation involves placing the filters on the lower ends of the reaction tubes in the reservoir block wells, and the upper ends passing through the holder block apertures and into the manifold.

专利号:WO-0146695-A1
优先权日:1999-12-08
标 题:Novel supports for solid phase synthesis
发明人:ANTONENKO VALERY V; THIELE JOCHEN; ATUEGBU ANDY E
权利人:GLAXO GROUP LTD; ANTONENKO VALERY V; THIELE JOCHEN; ATUEGBU ANDY E
摘要:Novel solid supports and methods for their use in the synthesis of chemical compounds by the sequential addition of chemical building blocks are provided. The solid support comprises a polymer having reactive groups (for example, poly(styrene-co-vinylbenzyl chloride)) grafted to a chemically inert bulk material (such as a Teflon® membrane).
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✅ COA系统入驻 | 共享模式

主要参考文献


1: Chen C. Some pharmacokinetic aspects of the lipophilic terfenadine and zwitterionic fexofenadine in humans. Drugs R D. 2007;8(5):301-14. Review. Review. German. Review. Dutch. Review. Hungarian. Review. Review. Review. Review. Review. Review. Review. Review. Finnish. Review. Review. Review. Review. Review. Review. Review.

合成参考文献


参考文献:10.1186/1471-2377-5-22
摘要:Baraniuk JN, Casado B, Maibach H, Clauw DJ, Pannell LK, Hess S S. A Chronic Fatigue Syndrome - related proteome in human cerebrospinal fluid. BMC Neurol. 2005 Dec 01;5():22.
参考文献:10.2147/copd.s21071
摘要:Wilson R, Anzueto A, Miravitlles M, Arvis P, Faragó G, Haverstock D, Trajanovic M, Sethi S. A novel study design for antibiotic trials in acute exacerbations of COPD: MAESTRAL methodology. Int J Chron Obstruct Pulmon Dis. 2011;6():373–83.
参考文献:10.1002/rcm.5111
摘要:Flynn CA, Alnouti Y, Reed GA. Quantification of the transporter substrate fexofenadine in cell lysates by liquid chromatography/tandem mass spectrometry. Rapid Commun Mass Spectrom. 2011 Aug 30;25(16):2361–6.
参考文献:10.2165/11207520-000000000-00000
摘要:Perry CM. Eribulin. Drugs. 2011 Jul 09;71(10):1321–31. doi: 10.2165/11207520-000000000-00000.
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