CAS: 52093-21-7; (2R,3R,4R,5R)-2-(((1S,2S,3R,4S,6R)-4,6-Diamino-3-(((2R,3R,6S)-3-Amino-6-((Methylamino)Methyl)Tetrahydro-2H-Pyran-2-yl)Oxy)-2-Hydroxycyclohexyl)Oxy)-5-Methyl-4-(Methylamino)Tetrahydro-2H-Pyran-3,5-Diol

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CAS号32385-11-8 西索米星

📜西索米星 以 水 作为反应溶剂,化学反应 20.0H,反应生成 庆大霉素,小诺霉素
参考文献:Biotransformation Of Sisomicin And Verdamicin Bymicromonospora Sagamiensis
标题:Biotransformation Of Sisomicin And Verdamicin Bymicromonospora Sagamiensis
摘要:研究发现,一种 2-脱氧链霉胺白痴化突变体(micromonospora Sagamiensis)的静止细胞能将西索米星转化为庆大霉素 C1A 和沙加米星.通过离子交换和碳柱色谱相结合的方法分离了生物转化产物,并进行了适当的鉴定.在转化产物中没有检测到抗生素 G-52(6'-N-甲基西索米星).庆大霉素 C1A 在生物转化的早期形成,随后形成了沙加米星.西索米星可能首先发生(4',5')还原,然后是 6'-N-甲基化.通过使用类似的程序,证明了维达米星转化为庆大霉素 C2A(庆大霉素 C2 的 6'-C外嵌体),C2,然后是 C1.碳液相色谱法清楚地分离了庆大霉素 C2A,C2 和维达米星.在这一生物转化过程中,首先发生的是维达米星的(4',5')还原反应,然后是 6'-C-表聚反应,最后是 6'-N-甲基化反应.与萨加米菌相反,锡安菌 Nrrl5466 和伊代菌 Nrrl3292 不具有任何可检测到的西索米星或维达米星(4',5')还原活性.另外,Nrrl5466 将西索米星转化为抗生素 G-52,将维达米星转化为一种新的抗生素 Vf3-1.根据色谱和质谱数据,抗生素 Vf3-1 被认为是 6'-N-甲基氟达米星.讨论了这些发现对相思豆菌中沙加米星生物合成的影响.
DOI:10.1080/00021369.1982.10865090

专利信息

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:WO-2009094569-A2
优先权日:2008-01-25
标 题:Method for the enzymatic kinetic resolution of acyloxyalkyl thiocarbonates used for the synthesis of acyloxyalkyl carbamates

专利号:US-2005222431-A1
优先权日:2003-12-30
标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof