CAS: 58152-03-7; (S)-3-Amino-N-((1R,2S,3S,4R,5S)-5-Amino-4-(((2R,3R,4S,5S,6R)-6-(Aminomethyl)-3,4,5-Trihydroxytetrahydro-2H-Pyran-2-yl)Oxy)-2-(((2R,3R,4R,5R)-3,5-Dihydroxy-5-Methyl-4-(Methylamino)Tetrahydro-2H-Pyran-2-yl)Oxy)-3-Hydroxycyclohexyl)-2-Hydroxypropanamide

该化合物是一种半合成的微粒素抗生素,来自二色丙烯,其结构表现为对古丁阴性细菌和一些古丁阳性细菌的广谱活动,其结构以1-N-(S)-3-氨-2-羟丙基丙基丙基酰侧链为主,加强了对许多微粒色色调的酶的稳定性,减少了抗药性发展.异丙胺显示出对诸如Pseudomonas aeruginosa,Escherichira coli和Klebsiella肺炎等病原体的强大功效,包括耐其他微粒性细菌的菌株,其致癌特征包括可靠的组织渗透和有利的安全比值,与早期的微粒色表面相比,其...

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46H61O18N5C46H61O18N5 3,6'-bis-N-benzyloxycarbonylgentamicin B sisomicin 6-azido-2,3,4-tri-O-benzyl-6-deoxy-α-D-glucopyranosyl chloride6'-N-(t-butoxycarbonyl)-isepamicin 6'-N-benzyloxycarbonyl-isepamicin 6'-N-(t-butoxycarbonyl)-3'''-N-(benzyloxycarbonyl)isepamicin 3,6',3''-tri-N-(t-butoxycarbonyl)-isepamicin

合成工艺路线路线简述

    📜西索米星置于palladium On Activated Charcoal 4 A Molecular Sieve,Tea,硫酸,Zinc Diacetate,氢气,Silver Trifluoromethanesulfonate,1-羟基苯并三唑,三乙胺,N,N'-二环己基碳二亚胺体系中,用 四氢呋喃,1,4-二氧六环,甲醇,苯 作为反应溶剂,化学反应 17.0H,反应生成 异帕米星
    参考文献:A Semisynthesis Of Isepamicin By Fragmentation Method
    标题:A Semisynthesis Of Isepamicin By Fragmentation Method
    摘要:Garamine Derivative,Key Intermediate,Was Obtained From Acid Cleavage Of Sisomicin Derivative. Its Subsequent Product Was Glycosylated With 6-Azido-2,3,4-Tri-O-Benzyl-6-Deoxy-Alpha-D-Glucopyranosyl Chloride Using Silver Triflate As A Promoter To Give Isepamicin. (C) 2004 Elsevier Ltd. All Rights Reserved.
    DOI:10.1016/j.Tetlet.2004.11.130

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    专利信息


    专利号:US-10925977-B2
    优先权日:2006-10-05
    标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
    发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
    权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
    摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

    专利号:US-8147805-B2
    优先权日:2005-01-05
    标题:Conjugates for dual imaging and radiochemotherapy: composition, manufacturing, and applications
    发明人:YANG DAVID; YU DONGFANG; CHANDA MITHU; AZHDARINIA ALI; OH CHANGSOK; KIM E EDMUND
    权利人:YANG DAVID; YU DONGFANG; CHANDA MITHU; AZHDARINIA ALI; OH CHANGSOK; KIM E EDMUND; UNIV T EXAS SYSTEM BOARD OF REGENTS
    摘要:Compositions and methods for dual imaging and for dual chemotherapy and radiotherapy are disclosed. More particularly, the invention concerns compounds comprising the structure X 1 —Y—X 2 , wherein Y comprises two or more carbohydrate residues covalently attached to one another, X 1 and X 2 are diagnostic or therapeutic moieties covalently attached to Y, provided that when Y does not comprise a glucosamine residue, X 1 and X 2 are diagnostic moieties. The present invention also concerns methods of synthesis of these compounds, application of such compounds for dual imaging and treatment of hyperproliferative disease, and kits for preparing a radiolabeled therapeutic or diagnostic compound.

    专利号:US-10472663-B2
    优先权日:2015-01-21
    标 题:Procedure for the rapid determination of bacterial susceptibility to antibiotics that inhibit protein synthesis
    发明人:FERNÃ?NDEZ GARCÃ?A JOSÉ LUIS; GOSÃ?LVEZ BERENGUER JAIME; BOU ARÉVALO GERMÃ?N; TAMAYO NOVAS MARIA; SANTISO BRANDARIZ REBECA; OTERO FARIÑA FÃ?TIMA MARÃ?A
    权利人:ABM TECH LLC
    摘要:The present invention relates to a method for the rapid evaluation of bacterial susceptibility or non-susceptibility of bacteria to antibiotics that inhibit protein synthesis. The rationale is to identify bacterial responses that depend or are influenced by protein synthesis. If this response is prevented or reduced by the antibiotic that inhibits the protein synthesis, the bacteria are susceptible to this antibiotic. Otherwise, if the response keeps similar despite the incubation with the antibiotic, the bacteria are not susceptible or resistant to this antibiotic. These responses could be determined at the DNA lev-el, cell wall level, morphological level or any other experimental approach, including metabolic, bio-chemical, physiological or genetic processes.

    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.

    专利号:AU-2007308022-A2
    优先权日:2006-10-05
    标题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications

    专利号:AU-2007308022-A1
    优先权日:2006-10-05
    标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications

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    主要参考文献

    1. Barr WH, Colucci R, Radwanski E, Zampaglione N, Cutler D, Lin CC, Elliott M, Affrime MB. Pharmacokinetics of isepamicin. J Chemother. 1995 Jun;7 Suppl
    2:53-61. 38(3):205-23. doi: 10.2165/00003088-200038030-00002. 10(2):207-18. doi: 10.1586/eri.11.170.

    合成参考文献


    参考文献:10.1128/aac.01444-09
    摘要:Toth M, Frase H, Chow JW, Smith C, Vakulenko SB. Mutant APH(2'')-IIa enzymes with increased activity against amikacin and isepamicin. Antimicrob Agents Chemother. 2010 Apr;54(4):1590–5.
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