CAS: 64952-97-2; Moxalactam

该化合物是属于甲状腺素类的合成乙型林丹抗生素,主要用于对各种克状阳性和克状阴性细菌的广谱抗菌活动,其特征为独特的双环结构,包括对其抗微生物作用至关重要的乙状腺环;该化合物一般通过注射进行,并因其稳定性而闻名其具有抗某些乙状腺素的稳定性,细菌产生的酶可以使许多抗生素不活跃;甲状腺活性氨具有良好的组织渗透性,并能有效治疗呼吸道感染,皮肤感染和腹部内感染等传染病;其致癌性肿瘤包括相对短的半衰期,需要多剂量才能产生持续的治疗效果;不良效应可能包括过敏反应,胃肠扰动和对肾功能的潜在影响.

结构式图片

MSDS等安全信息

上下游产品

41H38N6O10SC41H38N6O10Sdecarboxy-moxalactam moxalactam (S)

合成工艺路线路线简述

    在 三氯乙酸体系中,用 苯酚 作为反应溶剂,化学反应 2.5H,反应生成 拉氧头孢
    参考文献:一种β-内酰胺类化合物羧基及羟基保护基脱除方法
    标题:一种β-内酰胺类化合物羧基及羟基保护基脱除方法
    摘要:本发明公开了一种β‑内酰胺类化合物羧基及羟基保护基脱除方法,该方法是将羧基和/或羟基被保护的β‑内酰胺类化合物在三氯乙酸和碳正离子吸收剂作用下脱除保护基得到β‑内酰胺化合物脱保护的产物.本发明方法采用三氯乙酸代替三氟乙酸,且三氯乙酸和苯酚或间甲酚,苯甲醚联用,可以大大减少三氯乙酸的用量;此外,三氯乙酸在后续头孢成钠盐过程中遇水会分解成氯仿和二氧化碳,易于除去,不存在三氯乙酸残余的问题,反应产率高,杂质相对较少;三氯乙酸价格便宜且环保,降低成本有利于工业化生产.

    海关参考信息

    专利信息


    专利号:US-2005186197-A1
    优先权日:2002-08-29
    标 题:Peptide inhibitors of beta lactamases
    发明人:PALZKILL TIMOTHY; HUANG WANZHI
    摘要:Peptide inhibitors of β-lactamases have been identified by the synthesis of peptide arrays using synthesis SPOT technology. These peptide inhibitors of β-lactamase have activity against a broad spectrum of β-lactamases and are useful in a variety of applications.

    专利号:US-8017776-B2
    优先权日:2003-07-15
    标题 :Methods for synthesis of acyloxyalkyl compounds
    发明人:BHAT LAXMINARAYAN; GALLOP MARK A
    权利人:XENOPORT INC
    摘要:Disclosed herein are methods for synthesizing 1-(acyloxy)-alkyl prodrug derivatives of drugs through oxidation of 1-acyl-alkyl derivatives of drugs under anhydrous reaction conditions. The methods typically proceed stereospecifically, in high yield, do not require the use of activated intermediates and/or toxic compounds and are readily amenable to scale-up.

    专利号:US-8143437-B2
    优先权日:2002-02-19
    标题:Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof
    发明人:GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X
    权利人:GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X; XENOPORT INC
    摘要:The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require the use of activated intermediates and/or toxic compounds and is readily amendable to scale-up. The current invention also provides 1-acyl-alkyl derivatives of known drug components and methods for synthesizing these 1-acyl-alkyl derivatives.

    专利号:US-2025002508-A1
    优先权日:2020-05-05
    标题 :Boronic acid derivatives and synthesis, polymorphic forms, and therapeutic uses thereof
    发明人:HECKER SCOTT J; BOYER SERGE HENRI; BIO MATTHEW M; FANG YUANQING; GONZALES DE CASTRO ANGELA; LEFORT LAURENT; ZHU ZUOLIN; LINDER THOMAS
    权利人:QPEX BIOPHARMA INC
    摘要:Disclosed herein are antimicrobial compounds, polymorphic forms, compositions, pharmaceutical compositions, the method of use and preparation thereof. Some embodiments relate to boronic acid derivatives and their use as therapeutic agents, for example, β-lactamase inhibitors (BLIs).

    专利号:US-2005239725-A1
    优先权日:2002-02-19
    标题:Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof

    专利号:US-11135200-B2
    优先权日:2014-12-20
    标题:Antimicrobial drug synthesis and therapeutic compositions
    发明人:GREGG JOHN MALCOLM HALL
    权利人:GREGG JOHN MALCOLM HALL
    摘要:This invention relates to the medical use of an antimicrobial agent, racemic Ornidazole, its (R) and (S) enantiomers, or pharmaceutically acceptable salts or esters thereof, and to methods of treatment which involve treating a subject with Ornidazole. The racemic (rac)-ornidazole, its enantiomers, or pharmaceutically acceptable salts or esters thereof, may be used in combination with other actives. The invention also relates to pharmaceutical formulations and compositions comprising (rac)-ornidazole, (R)-ornidazole, (S)-ornidazole, or pharmaceutically acceptable salts or esters thereof, and/or other actives as well as methods to stereoselectively manufacture the enantiomers.
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    主要参考文献


    1: Chen P, Zhang E, Ma Y, Xiong L, Chen Y, Shen P, Ji J, Ying C, Liu Z, Xiao Y. Time to Awaken a Forgotten Antibacterial Agent: A 10-year Nationwide Surveillance of Latamoxef Resistance in China Based on 46,716 Isolates and Establishment of Tentative Epidemiological Cut-Off Values. Infect Drug Resist. 2026 Feb 23;19:566382. doi: 10.2147/IDR.S566382.
    2: Li S, Ding P, Wang C, Long K, Gao P. ATAK complex (adrenaline, takotsubo, anaphylaxis, and kounis hypersensitivity-associated coronary syndrome) related to latamoxef administration-a case report. Front Cardiovasc Med. 2024 Jul 22;11:1383903. doi: 10.3389/fcvm.2024.1383903.
    3: Kusumoto M, Narita H, Motegi T, Harada K. Estimation of latamoxef (moxalactam) dosage regimens against β-lactamase-producing Enterobacterales in dogs: a pharmacokinetic and pharmacodynamic analysis using Monte Carlo simulation. J Vet Med Sci. 2024 Aug 2;86(8):841-846. doi: 10.1292/jvms.24-0197. Epub 2024 Jun 18.

    合成参考文献


    摘要:S55 | ZINC15PHARMA | Pharmaceuticals from ZINC15 | DOI:10.5281/zenodo.3247749
    摘要:Kleemann, A.; Engel, J.; Kutscher, B.; Reichert, D., Pharmaceutical Substances[Online], Thieme: Stuttgart, (2003).
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