CAS: 125602-71-3; (S)-4-(4-((4-Chlorophenyl)(Pyridin-2-yl)Methoxy)Piperidin-1-yl)Butanoic Acid

该化合物是一种主要用于治疗过敏结膜炎和其他过敏条件的抗脊髓灰质炎药物,具有选择性的H1受体抗体抗争作用,有效阻止过敏反应的化合物 ----异丙胺 ----一种过敏反应的化合物. 众所周知,异丙胺是一种快速行动,与第一代抗脊髓灰质炎相比,镇静效应相对较低,因此适合用于需要避免沉睡的病人.该物质通常作为一种眼科治疗方法进行施用,允许直接应用于受影响地区.其化学结构包括一个管状菌环,有助于其药理学特性. 青蒿素一般受到良好的调剂,副作用较低,尽管一些病人在施用时可能受到当地温和的刺激或不适. 与任何药物一样,用户必须遵循处方剂量,并就与其他药物或基本健康状况的潜在互动情况咨询保健专业人员.

结构式图片

上下游产品

Bepotastine
Ethyl (S)-4-[4-[(4-Chlorophenyl)(2-Pyridyl)Methoxy]Piperidino]Butanoate
(S)-2-[(4-氯苯基)(4-哌啶氧基)甲基]吡啶 (S)-(-)-4-[(4-Chlorophenyl)(2-Pyridyl)Methoxy]Piperidine 201594-84-5
2-[(4-氯苯基)(4-哌啶基氧基)甲基]吡啶 2-((4-Chlorophenyl)(Piperidin-4-Yloxy)Methyl)Pyridine 122368-54-1
4-[(4-氯苯基)-2-吡啶基甲氧基]-1-哌啶甲酸乙酯 Ethyl 4-((4-Chlorophenyl)(Pyridin-2-yl)Methoxy)Piperidine-1-Carboxylate 207726-35-0
(S)-Bepotastine L-Menthyl Ester 1092777-17-7
(Rs)-4-[4-[(4-Chlorophenyl)(2-Pyridyl)Methoxy]Piperidino]Butyric Acid D-Menthyl Ester 1560797-65-0
(S)-4-[4-[(4-Chlorophenyl)(2-Pyridyl)Methoxy]Piperidino] Butyric Acid D-Menthyl Ester 1560797-69-4 (4-Chlorophenyl)(Pyridin-2-yl)Methyl 2,2,2-Trichloroacetimidate (S)-(4-Chlorophenyl)(Pyridin-2-yl)Methanol 176022-47-2

合成工艺路线路线简述

    (S)-4-[4-[(4-Chlorophenyl)(2-Pyridyl)Methoxy]Piperidin-1-Yl]Butyramide置于水,Sodium Hydroxide体系中,用 乙醇 用作溶剂,以96%的收率获得贝托斯汀
    参考文献:一种抗过敏药物贝他斯汀的制备方法
    标题:一种抗过敏药物贝他斯汀的制备方法
    摘要:本发明公开了一种抗过敏药物贝他斯汀的制备方法,属于抗过敏药物的合成技术领域.本发明的技术方案要点为:以化合物(S)‑(4‑氯苯基)(2‑吡啶基)‑甲醇式(式ii)为起始原料与n‑叔丁氧羰基‑4卤哌啶反应得到化合物(S)‑n‑叔丁氧羰基‑4‑[(4‑氯苯基)(2‑吡啶基)甲氧基]哌啶(式iii);在酸性条件下脱除式(III)化合物的保护基得到化合物(S)‑4‑[(4‑氯苯基)(2‑吡啶基)甲氧基]哌啶式(iv);式(iv)化合物与4‑卤丁酰胺再经亲核取代反应得到化合物(S)‑4‑[(4‑氯苯基)(2‑吡啶基)甲氧基]‑哌啶基]‑丁酰胺(式v),最后式(v)化合物的酰胺基团水解得到目标产物抗过敏药物贝他斯汀.本发明的合成路线简单且成本低廉,适合规模化生产光学纯抗过敏药物贝他斯汀.

    海关参考信息

    专利信息


    专利号:WO-2023075715-A1
    优先权日:2021-10-26
    标题 :A pharmaceutical formulation including leukotriene receptor antagonists and/or leukotriene synthesis inhibitors combined with non-steroidal anti-inflammatory drugs (nsaids)
    发明人:OYTUN FARUK; CAN EFE
    权利人:VSY BIYOTEKNOLOJI VE ILAC SANAYI ANONIM SIRKETI
    摘要:This invention is related to a pharmaceutical formulation including Leukotriene receptor antagonists and/or Leukotriene synthesis inhibitors combined with non-steroidal anti-inflammatory drugs (NSAIDs) and antihistamines in ocular diseases and in inflammatory and allergic diseases for systemic and topical use. The objective of this invention is to create a novel formulation to be effective as much as steroids while having significantly less side effects for long-term use in treating ocular diseases, inflammatory and allergic diseases. In other words our aim is to achieve the inhibition of pro-inflammatory mediators (prostaglandins, thromboxane, histamine and leukotrienes) as much as steroids do with a safer combination.

    专利号:CN-111100851-A
    优先权日:2018-10-25
    标 题:Alcohol dehydrogenase mutant and application thereof in synthesis of chiral diaryl alcohol compound

    专利号:CN-103121966-A
    优先权日:2011-11-17
    标题:Directional synthesis of (4-chlorophenyl)-(pyridin-2-yl)-methanol

    专利号:CN-111100851-B
    优先权日:2018-10-25
    标题:Alcohol dehydrogenase mutants and their application in the synthesis of chiral biaryl alcohol compounds

    专利号:CN-107827812-A
    优先权日:2017-11-23
    标 题 :A kind of chiral synthesis method of bepotastine benzenesulfonate intermediate

    专利号:CN-106938995-B
    优先权日:2017-01-17
    标题:A kind of asymmetric synthesis method of ophthalmic drug bepotastine besylate
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    主要参考文献


    1: Yoon S, Jin BH, Kim CO, Park K, Park MS, Chae D. Pharmacokinetic Modeling of Bepotastine for Determination of Optimal Dosage Regimen in Pediatric Patients with Allergic Rhinitis or Urticaria. Pharmaceutics. 2024 Feb 27;16(3):334. doi: 10.3390/pharmaceutics16030334.
    2: Kitahiro Y, Yamamoto K, Yakushijin K, Ioroi T, Tanda M, Itohara K, Omura T, Minami H, Yano I. The Efficacy of Bepotastine Besilate Compared With Hydroxyzine Pamoate for Preventing Infusion Reactions to the First Dose of Rituximab in Patients With Non-Hodgkin Lymphoma: Protocol for a Phase II, Double-Blind, Multicenter Randomized Trial. JMIR Res Protoc. 2024 Feb 22;13:e54882. doi: 10.2196/54882.
    3: Marini MC, Berra ML, Girado F, Albera PA, Del Papa MS, Passerini MS, Aguilar AJ. Efficacy and Toxicity Evaluation of Bepotastine Besilate 1.5% Preservative- Free Eye Drops Vs Olopatadine Hydrochloride 0.2% Bak-Preserved Eye Drops in Patients with Allergic Conjunctivitis. Clin Ophthalmol. 2023 Nov 16;17:3477-3489. doi: 10.2147/OPTH.S431889.
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