CAS: 830-89-7; Albutoin

相似化合物

436855-68-4 53517-95-6 55523-05-2

📜Dl-亮氨酸置于吡啶,水,达卡巴嗪,三乙胺,N,N-二异丙基乙胺体系中,用 二氯甲烷,水,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 28.0H,反应生成 阿布妥因
参考文献:Thiourea Modified Doxorubicin: A Perspective Ph-Sensitive Prodrug
标题:Thiourea Modified Doxorubicin: A Perspective Ph-Sensitive Prodrug
摘要:提出了一种合成ph敏感前药的新方法:硫脲药物修饰.由此产生的前药能在肿瘤细胞酸性环境中释放出细胞毒素和生物活性2-硫乙内酰脲.通过fret模型验证了硫脲在酸性催化下环化成2-硫乙内酰脲的概念.获得了模型叠氮胸苷,细胞毒素阿霉素和2-硫乙内酰脲阿布妥因的双前药,在酸性环境中能释放相应的药物.对前列腺癌细胞进行了所得阿霉素前药的测试,结果显示硫脲修饰的前药在ph 7.6中性环境下比阿霉素(ic50范围为0.01258至0.02559 μm)的细胞毒性低(平均ic50范围为0.5584至0.9885 μm),而在癌细胞的轻度酸性条件下与阿霉素(ic50范围为0.2303至0.8110 μm)的毒性相似(平均ic50范围为0.4970至0.7994 μm).在pc3肿瘤细胞中,Dox前药的细胞内和核内积累远远高于游离阿霉素.
DOI:10.1021/acs.Bioconjchem.8B00885

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-8017776-B2
优先权日:2003-07-15
标题 :Methods for synthesis of acyloxyalkyl compounds
发明人：BHAT LAXMINARAYAN; GALLOP MARK A
权利人:XENOPORT INC
摘要:Disclosed herein are methods for synthesizing 1-(acyloxy)-alkyl prodrug derivatives of drugs through oxidation of 1-acyl-alkyl derivatives of drugs under anhydrous reaction conditions. The methods typically proceed stereospecifically, in high yield, do not require the use of activated intermediates and/or toxic compounds and are readily amenable to scale-up.

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-2008214827-A1
优先权日:2004-02-03
标 题:Synthesis of Cyanoimino-Benzoimidazoles
发明人：GOEHRING R RICHARD; WHITEHEAD JOHN; SHAO BIN
权利人:EURO CELTIQUE SA
摘要:Disclosed in certain embodiments is a process for synthesizing a compound of formula (V) and salts thereof.

专利号:US-8143437-B2
优先权日:2002-02-19
标题:Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof
发明人：GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X
权利人:GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X; XENOPORT INC
摘要:The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require the use of activated intermediates and/or toxic compounds and is readily amendable to scale-up. The current invention also provides 1-acyl-alkyl derivatives of known drug components and methods for synthesizing these 1-acyl-alkyl derivatives.

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