CAS: 13412-64-1; Sodium (2S,5R,6R)-6-(3-(2,6-Dichlorophenyl)-5-Methylisoxazole-4-Carboxamido)-3,3-Dimethyl-7-Oxo-4-Thia-1-Azabicyclo[3.2.0]Heptane-2-Carboxylate Hydrate

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合成工艺路线路线简述

    三乙胺,尿素,6-氨基青霉烷酸,三甲基氯硅烷,3-(2',6'-Dichlorophenyl)-5-Methyl-4-Isoxazolyl Chloride,钠,Sodium 2-Ethylhexanoic Acid,置于水,Sodium Sulfate-Iii,丙酮体系中,用 二氯甲烷,丙酮,水 用作溶剂,化学反应 3.92H,以to Yield 93.0 G Of Sodium Dicloxacillin Monohydrate (91.2% Of The Theoretical Amount),As A White,Crystalline Powder的收率获得双氯西林钠
    参考文献:Manufacture Of Semi-Synthetic Penicillin Antibiotics
    标题:Manufacture Of Semi-Synthetic Penicillin Antibiotics
    摘要:本文描述了改进或与半合成青霉素抗生素的制造有关的改进.更具体地讲,本文描述了一种改进的过程,用于制备6-β-酰氨基青霉烷酸抗生素产品,其中6-β-氨基青霉烷酸(6-Apa)在惰性溶剂中与硅基化剂反应,形成式(I)的硅化化合物:##str1## 其中r.Sup.1代表氢原子或三(c.Sub.1-6烷基)硅基基团,R.Sup.2代表三(c.Sub.1-6烷基)硅基基团,然后将式(I)的化合物与相应于所需6-β-酰氨基基团的酰氯或受保护的酰氯接触,裂解硅基团并回收所需的抗生素产品,硅化作用使用三(c.Sub.1-6烷基)硅基脲或三(c.Sub.1-6烷基)卤代硅烷进行,产生的式(I)的化合物在无中间分离的情况下与酰氯或受保护的酰氯反应,其中酰基化在存在氢卤化物受体混合物的情况下进行,所述混合物包括超过0.15摩尔和优选为每摩尔6-Apa的3.00摩尔的脲;超过0.15摩尔和优选为每摩尔6-Apa的1.30摩尔的双三(c.Sub.1-6烷基)硅基脲;以及超过0.25摩尔和优选为每摩尔6-Apa的3.30摩尔的三(c.Sub.1-6烷基)铵卤化物.该过程特别适用于高产量和高纯度的氨苄青霉素和阿莫西林的制备.

    海关参考信息

    专利信息


    专利号:US-2024197774-A1
    优先权日:2021-04-16
    标 题:Synthesis of Antimicrobial PVP-coated Bismuth Nanoparticles
    发明人:LOPEZ-RIBOT JOSE; VAZQUEZ-MUNOZ ROBERTO
    权利人:UNIV TEXAS
    摘要:Described herein is a facile, fast, and economical method for the synthesis of BAL-mediated PVP-BiNPs, using basic laboratory instruments and reagents readily available in most laboratories.

    专利号:US-8557979-B2
    优先权日:2004-06-10
    标题 :Carbapenem antibacterials with gram-negative activity and processes for their preparation
    发明人:CHOI WOO-BAEG; KOWALIK EWA
    权利人:CHOI WOO-BAEG; KOWALIK EWA; FOB SYNTHESIS INC
    摘要:The present invention provides β-methyl carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment. The present invention is also in the field of synthetic organic chemistry and is specifically provides an improved method of synthesis of β-methyl carbapenems which are useful as antibacterial agents.

    专利号:US-10933051-B2
    优先权日:2017-06-09
    标 题 :Carbapenem compounds and compositions for the treatment of bacterial infections
    发明人:CHOI WOO-BAEG; TOMIOKA TAKASHI; JOO HYUNG-YEUL; TRUONG PHONG; MIN BRIAN
    权利人:FOB SYNTHESIS INC
    摘要:The present invention provides carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections, including drug resistant or multiple-drug resistant bacterial infections, and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment.

    专利号:US-9693999-B2
    优先权日:2011-01-26
    标题:Small molecule RNase inhibitors and methods of use
    发明人:DUNMAN PAUL M; OLSON PATRICK D; CHILDERS WAYNE
    权利人:UNIV ROCHESTER; UNIV NEBRASKA; Temple University—Of the Commonwealth System of Higher Education
    摘要:Small molecule inhibitors of bacterial ribonuclease (e.g., RnpA) and methods for their synthesis and use are described herein. The methods of using the compounds include treating and preventing microbial infections and inhibiting bacterial ribonuclease. Also described herein are methods of identifying compounds for treating or preventing a microbial infection.

    专利号:US-9937151-B2
    优先权日:2010-06-18
    标题 :Carbapenem antibacterials with gram-negative activity
    发明人:CHOI WOO-BAEG; GRUSZECKA-KOWALIK EWA; JOO HYUNG-YEUL; LIU SHUANGPEI; MAO SHULI; LI YONGFENG; KIM DEOG-IL
    权利人:FOB SYNTHESIS INC
    摘要:The present invention provides β-methyl carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment.

    专利号:WO-2009056955-A1
    优先权日:2007-10-30
    标题 :Amine-bearing phospholipids (abps), their synthesis and use
    发明人:ZUMBUEHL ANDREAS
    权利人:UNIV BASEL; ZUMBUEHL ANDREAS
    摘要:Disclosed herein are amine-bearing phospholipids (ABP). The ABPs display many properties and functionalities of naturally occurring phospholipids, but also new properties and functionalities, such as the ability to polymerize while maintaining structural integrity, that may supplement or expand the functionalities of naturally occurring phospholipids.
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    主要参考文献


    1: Naguib IA, Abdelaleem EA, Zaazaa HE, Hussein EA. Partial Least-Squares and Linear Support Vector Regression Chemometric Methods for Simultaneous Determination of Amoxicillin Trihydrate and Dicloxacillin Sodium in the Presence of Their Common Impurity. J AOAC Int. 2016 Jul;99(4):972-979. doi: 10.5740/jaoacint.16-0033. Epub 2016 Jun 15. doi: 10.2147/DDDT.S92117. eCollection 2015.
    3: Acharya DR, Patel DB. Development and Validation of RP-HPLC Method for Simultaneous Estimation of Cefpodoxime Proxetil and Dicloxacillin Sodium in Tablets. Indian J Pharm Sci. 2013 Jan;75(1):31-5. doi: 10.4103/0250-474X.113538.
    4: Dhoka MV, Sandage SJ, Dumbre SC. Simultaneous determination of cefixime trihydrate and dicloxacillin sodium in pharmaceutical dosage form by reversed-phase high-performance liquid chromatography. J AOAC Int. 2010 Mar-Apr;93(2):531-5. Epub 2006 Nov 27. Polish.

    合成参考文献


    摘要:Japanese Journal of Antibiotics., 21(274), 1968 []
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