Fortimicin A tetrahydr°Chloride(R)-2-Amino-N-{(1S,2R,3R,4S,5S,6R)-4-amino-3-[(2R,3R,6S)-3-amino-6-(1-amino-ethyl)-tetrahydro-pyran-2-yloxy]-2,5-dihydroxy-6-methoxy-cyclohexyl}-N-methyl-propionamide; hydr°Chloride(S)-2-Amino-N-{(1S,2R,3R,4S,5S,6R)-4-amino-3-[(2R,3R,6S)-3-amino-6-(1-amino-ethyl)-tetrahydro-pyran-2-yloxy]-2,5-dihydroxy-6-methoxy-cyclohexyl}-N-methyl-propionamide; hydr°Chloridefortimicin A tetrahydr°ChlorideN-{(1S,2R,3R,4S,5S,6R)-4-Amino-3-[(2R,3R,6S)-3-amino-6-(1-amino-ethyl)-tetrahydro-pyran-2-yloxy]-2,5-dihydroxy-6-methoxy-cyclohexyl}-N-methyl-acetamide; hydr°Chloride
合成工艺路线路线简述
📜Fortimicin A Tetrahydrochloride置于anion-Exchange Column体系中,化学反应生成 阿司米星,Fortimicin B 参考文献:2'-N-酰基fortimicins和2'-N-烷基fortimicins通过异fortimicin重排1 标题:2'-N-酰基fortimicins和2'-N-烷基fortimicins通过异fortimicin重排1 摘要:摘要fortimicin A和许多4-N-酰基fortimicins B虽然可以作为完全质子化的盐酸盐或硫酸盐稳定,但在水溶液中会以游离碱的形式降解.对fortimicin A和4-N-乙酰福寿霉素b进行的详细研究表明,降解发生的部分原因是通过形成fortimicin B的4-N-酰基的简单裂解,以及部分地通过重排至2'-N-酰基fortimicins B(isofortimicin重排).描述了将重排产物转化为2'-N-甘氨酰香豆素a,2'-N-乙酰香豆素a和2'-N-(2-氨基乙基)香豆素a和b的转化.介绍了新的fortimicin A衍生物的抗菌活性. DOI:10.1016/s0008-6215(00)84564-4
专利号:US-9353057-B2 优先权日:2003-12-30 标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof 发明人:GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA 权利人:XENOPORT INC 摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.
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-2015158809-A9 优先权日:2013-02-26 标 题 :Method of making 1-(acyloxy)-alkyl carbamate compounds 发明人:WANG HUAN; LIU PENG; DAI QUNYING; YIN HAO; RAILLARD STEPHEN P 权利人:XENOPORT INC 摘要:Methods of preparing carbamate prodrugs of amine-containing drugs are provided. Carbonates useful in the synthesis of the carbamate prodrugs are also provided.
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-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.
1: Huong NL, Hoang NH, Hong SY, Sohng JK, Yoon YJ, Park JW. Characterization of fortimicin aminoglycoside profiles produced from Micromonospora olivasterospora DSM 43868 by high-performance liquid chromatography-electrospray ionization-ion trap-mass spectrometry. Anal Bioanal Chem. 2016 Feb;408(6):1667-78. doi: 10.1007/s00216-015-9281-2. Epub 2016 Jan 11. Chinese. Epub 2007 Apr 7. 5: Boehr DD, Jenkins SI, Wright GD. The molecular basis of the expansive substrate specificity of the antibiotic resistance enzyme aminoglycoside acetyltransferase-6'-aminoglycoside phosphotransferase-2". The role of ASP-99 as an active site base important for acetyl transfer. J Biol Chem. 2003 Apr 11;278(15):12873-80. Epub 2003 Feb 3. Japanese. Japanese. 13: Rogers J, Davies J. The pseudodisaccharides: a novel class of group I intron splicing inhibitors. Nucleic Acids Res. 1994 Nov 25;22(23):4983-8. Erratum in: Nucleic Acids Res 1995 Feb 11;23(3):540.
合成参考文献
参考文献:10.1007/bf00279641 摘要:Dairi T, Ohta T, Hashimoto E, Hasegawa M. Organization and nature of fortimicin A (astromicin) biosynthetic genes studied using a cosmid library of Micromonospora olivasterospora DNA. Molecular Genetics and Genomics. 1992 Dec;236(1):39–48. doi: 10.1007/bf00279641. 参考文献:10.1007/bf00279642 摘要:Dairi T, Yamaguchi K, Hasegawa M. N-Formimidoyl fortimicin A synthase, a unique oxidase involved in fortimicin A biosynthesis: purification, characterization and gene cloning. Molecular Genetics and Genomics. 1992 Dec;236(1):49–59. doi: 10.1007/bf00279642.