CAS: 51756-80-0; 3-Amino-Rifamycin S

该化合物是S类离子胺素的半合成衍生物,主要用作合成抗微生物剂的中间体,其技术级配方确保适合工业规模的应用,特别是在药物研究和生产方面.该复合物展示了反应性氨基体组,能够进一步进行化学改造以开发以离子素为基础的抗生素.关键优势包括:在受控条件下其高纯度和稳定性,有利于下游工艺的一致性能.作为前体,它在开发具有强化抗菌特性的强效离子素类中发挥着关键作用.建议适当处理和储存以保持合成应用的完整性.

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rifamycin S rifamycin SV N-(4-ntrobenzyloxycarbonyl)-3-aminorifamycin S

合成工艺路线路线简述

    3-Amino-Rifamycin,二氧化锰 反应生成 3-Aminorifamycin S
    参考文献:Rossetti,V.;Marsili,L.;Pasqualucci,C.
    标题:Rossetti,V.;Marsili,L.;Pasqualucci,C.

    海关参考信息

    专利信息


    专利号:US-4743619-A
    优先权日:1985-08-29
    标 题 :Method of treating hepatitis
    发明人:HUNG PAUL P
    权利人:AMERICAN HOME PROD
    摘要:The invention disclosed herein provides a method of treating an animal infected by hepatitis B virus comprising administering to such infected animal an amount of a rifamycin derivative selected from a group consisting of (a) 3-amino-4-deoxo-4-imino-rifamycin S, (b) 3-amino-4-deoxo-4-[(4-aminophenyl)sulfonyl]amino-rifamycin SV, (c) 4-O-(n-butylsulfonyl)-3-[(1-piperidinylimino)methyl]-rifamycin SV, (d) 4-O-(n-butylsulfonyl)-3-[(4-morpholinylimino)methyl]-rifamycin SV, (e) 3-[(dimethylhydrazono)methyl]-4-O-[(3-phenylpropyl)sulfonyl]-rifamycin SV, and (f) 4-deoxo-N,3-ethylidenimino-4-(methylsulfonyl)amino-rifamycin SV, said amount being effective to alleviate the effects of said hepatitis B virus. Also disclosed is a method of inhibiting the viral polymerase of hepatitis B virus by subjecting said polymerase to an amount of one of the rifamycin derivatives (a)-(f) above, said amount being effective to prevent the synthesis of hepatitis B virus by said viral polymerase. Compounds (b)-(f) described above are novel compounds.

    专利号:US-4631290-A
    优先权日:1985-08-29
    标 题 :Method of treating hepatitis
    发明人:HUNG PAUL P
    权利人:AMERICAN HOME PROD
    摘要:The invention disclosed herein provides a method of treating an animal infected by hepatitis B virus comprising administering to such infected animal an amount of a rifamycin derivative selected from a group consisting of (a) 3-amino-4-deoxo-4-imino-rifamycin S, (b) 3-amino-4-deoxo-4-[(4-aminophenyl)sulphonyl]amino-rifamycin SV, (c) 4-O-n-butylsulphonyl-3-[(1-piperidinylimino)methyl]-rifamycin SV, (d) 4-O-n-butylsulfonyl-3-[(4-morpholinylimino)methyl]-rifamycin SV, (e) 3-[(dimethylhydrazono)methyl]-4-O-[(3-phenylpropyl)sulfonyl]-rifamycin SV said amount being effective to alleviate the effects of said hepatitis B virus. Also disclosed is a method of inhibiting the viral polymerase of hepatitis B virus by subjecting said polymerase to an amount of one of the rifamycin derivatives (a)-(e) above, said amount being effective to prevent the synthesis of hepatitis B virus by said viral polymerase.
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    合成参考文献


    参考文献:10.1021/acs.orglett.6b03619
    摘要:Williams DE, Dalisay DS, Chen J, Polishchuck EA, Patrick BO, Narula G, Ko M, Av-Gay Y, Li H, Magarvey N, Andersen RJ. Aminorifamycins and Sporalactams Produced in Culture by a Micromonospora sp. Isolated from a Northeastern-Pacific Marine Sediment Are Potent Antibiotics. Org Lett. 2017 Feb 17;19(4):766–9. doi: 10.1021/acs.orglett.6b03619.
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