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    Oxazolidinone antibacterial compound
    1.
    发明授权
    Oxazolidinone antibacterial compound 有权
    恶唑烷酮抗菌化合物

    公开(公告)号：US09573910B2

    公开(公告)日：2017-02-21

    申请号：US15034878

    申请日：2014-07-28

    申请人： Lee Pharma Limited

    发明人： Raghu Mitra Alla ,  Ajay Kumar Dubey ,  Srinivas Reddy Mallepalli ,  Ramakrishna Reddy Pongilati

    IPC分类号： C07D263/20 ,  A61K31/5377

    CPC分类号： C07D263/20 ,  A61K31/5377 ,  C07B2200/07 ,  Y02A50/473 ,  Y02A50/481 ,  Y02A50/483

    摘要： The invention relates to novel oxazolidinone compound. More particularly, the invention relates to novel [(S)—N-[[3-[4-fluoro-3-morpholino phenyl]-2-oxooxazolidin-5-yl] methyl] acetamide] compound of Formula-I which was disclosed in Indian Patent Application No. 5063/CHE/2013 and corresponding PCT/IN2014/000018. The compound is a broad spectrum antimicrobial agent effective against Multi-Drug Resistant S. Maltophilia pathogen and a large number of gram positive and gram negative pathogens. The compound has shown excellent biological activities against S. Maltophilia which has developed resistance against a large number of antibiotics including some of the known and widely used oxazolidinone derivatives.

    摘要翻译： 本发明涉及新型恶唑烷酮化合物。 更具体地，本发明涉及式I的新的[（S）-N - [[3- [4-氟-3-吗啉代苯基] -2-氧代恶唑烷-5-基]甲基]乙酰胺]化合物 在印度专利申请No.5063 / CHE / 2013和相应的PCT / IN2014 / 000018中。 该化合物是一种广泛的抗菌药物，可有效抵抗多药耐药性马氏杆菌病原体和大量革兰氏阳性和革兰氏阴性病原体。 该化合物已经显示出对马耳他菌的优良生物活性，其对大量抗生素产生抗性，包括一些已知且广泛使用的恶唑烷酮衍生物。

    Process for preparation of Linezolid and its novel intermediates
    2.
    发明授权
    Process for preparation of Linezolid and its novel intermediates 有权
    利奈唑胺及其新型中间体的制备方法

    公开(公告)号：US09376407B2

    公开(公告)日：2016-06-28

    申请号：US13820568

    申请日：2012-02-21

    申请人： Raghu Mitra Alla ,  Ajay Kumar Dubey ,  Aruna Kumari Sirigiri ,  Naga Kama Kumar Mareedu

    发明人： Raghu Mitra Alla ,  Ajay Kumar Dubey ,  Aruna Kumari Sirigiri ,  Naga Kama Kumar Mareedu

    IPC分类号： C07D263/06 ,  C07D263/20 ,  C07D263/14 ,  C07D265/30 ,  C07D269/00 ,  C07D413/10 ,  A61K31/5377

    CPC分类号： C07D263/06 ,  A61K31/5377 ,  C07D263/14 ,  C07D263/20 ,  C07D265/30 ,  C07D269/00 ,  C07D413/10

    摘要： A novel process for preparing oxazolidinone antibacterial agent Linezolid including key intermediates of oxazolidinones comprising: reacting 3-fluoro-4-morpholinyl aniline with R-epichlorohydrin; carbonylation to form oxazolidinone derivative; acetylation of (5R)-5-(chloromethyl)-3-(3-fluoro-4-morpholinophenyl-oxazolidin-2-one with sodium acetate to get novel intermediate; hydrolysis of (R)-3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazolidinyl methyl acetate; mesylation of (R)-3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazolidinyl methanol; reaction of (R)-3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazolidinyl methyl methane sulphonate with potassium phthalimide; hydrolysis of (S)-3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazolidinyl methyl phthalimide with hydrazine hydrate; acetylation of (S)-3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazolidinyl methyl amine with acetic anhydride yields Linezolid in high yield.

    摘要翻译： 一种制备恶唑烷酮抗菌剂利奈唑胺的新方法，包括恶唑烷酮的关键中间体，包括：使3-氟-4-吗啉基苯胺与R-表氯醇反应; 羰基化形成恶唑烷酮衍生物; （5R）-5-（氯甲基）-3-（3-氟-4-吗啉代苯基 - 恶唑烷-2-酮与乙酸钠的乙酰化得到新的中间体;（R）-3-（3-氟-4- （R）-3-（3-氟-4-吗啉代苯基）-2-氧代-5-恶唑烷基甲醇的甲磺酰化;（R）-3-（ 3-（3-氟-4-吗啉代苯基）-2-氧代-5-恶唑烷基甲基甲磺酸盐与邻苯二甲酰亚胺钾的水解;（S）-3-（3-氟-4-吗啉代苯基）-2-氧代-5-恶唑烷基甲基邻苯二甲酰亚胺 与水合肼反应;（S）-3-（3-氟-4-吗啉代苯基）-2-氧代-5-恶唑烷基甲基胺与乙酸酐的乙酰化，以高产率得到利奈唑胺。

    NOVEL PROCESS FOR PREPARATION OF LINEZOLID AND ITS NOVEL INTERMEDIATES
    5.
    发明申请
    NOVEL PROCESS FOR PREPARATION OF LINEZOLID AND ITS NOVEL INTERMEDIATES 有权
    制备线粒体及其新型中间体的新方法

    公开(公告)号：US20130324719A1

    公开(公告)日：2013-12-05

    申请号：US13820568

    申请日：2012-02-21

    申请人： Raghu Mitra Alla ,  Ajay Kumar Dubey ,  Aruna Kumari Sirigiri ,  Naga Kama Kumar Mareedu

    发明人： Raghu Mitra Alla ,  Ajay Kumar Dubey ,  Aruna Kumari Sirigiri ,  Naga Kama Kumar Mareedu

    IPC分类号： C07D263/06

    CPC分类号： C07D263/06 ,  A61K31/5377 ,  C07D263/14 ,  C07D263/20 ,  C07D265/30 ,  C07D269/00 ,  C07D413/10

    摘要： A novel process for preparing oxazolidinone antibacterial agent Linezolid including key intermediates of oxazolidinones comprising: reacting 3-fluoro-4-morpholinyl aniline with R-epichlorohydrin; carbonylation to form oxazolidinone derivative; acetylation of (5R)-5-(chloromethyl)-3-(3-fluoro-4-morpholinophenyl-oxazolidin-2-one with sodium acetate to get novel intermediate; hydrolysis of (R)-3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazolidinyl methyl acetate; mesylation of (R)-3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazolidinyl methanol; reaction of (R)-3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazolidinyl methyl methane sulphonate with potassium phthalimide; hydrolysis of (S)-3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazolidinyl methyl phthalimide with hydrazine hydrate; acetylation of (S)-3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazolidinyl methyl amine with acetic anhydride yields Linezolid in high yield.

    摘要翻译： 一种制备恶唑烷酮抗菌剂利奈唑胺的新方法，包括恶唑烷酮的关键中间体，包括：使3-氟-4-吗啉基苯胺与R-表氯醇反应; 羰基化形成恶唑烷酮衍生物; （5R）-5-（氯甲基）-3-（3-氟-4-吗啉代苯基 - 恶唑烷-2-酮与乙酸钠的乙酰化得到新的中间体;（R）-3-（3-氟-4- （R）-3-（3-氟-4-吗啉代苯基）-2-氧代-5-恶唑烷基甲醇的甲磺酰化;（R）-3-（ 3-（3-氟-4-吗啉代苯基）-2-氧代-5-恶唑烷基甲基甲磺酸盐与邻苯二甲酰亚胺钾的水解;（S）-3-（3-氟-4-吗啉代苯基）-2-氧代-5-恶唑烷基甲基邻苯二甲酰亚胺 与水合肼反应;（S）-3-（3-氟-4-吗啉代苯基）-2-氧代-5-恶唑烷基甲基胺与乙酸酐的乙酰化，以高产率得到利奈唑胺。