CAS: 41708-72-9; 2-Amino-N-(2,6-Dimethylphenyl)Propanamide

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2-phthalimidopropiono-2',6'-xylidide α-bromopropionyl-2,6-dimethylaniline 2-iodo-2',6'-propionoxylidide [(2,6-dimethylphenyl)amin°Carbonyl-1-ethyl]chloride2-(2,2,5,5-tetramethyl-2,5-dihydro-3-pyrroline-3-carbonylamino)-N-(2,6-dimethylphenyl)-propionamide 20H28N3O3C20H28N3O3 (+)-T°Cainide (-)-T°Cainide

📜Alpha-溴代-N-(2,6-二甲基苯基)丙酰胺置于氨体系中,用 氯仿,水 作为反应溶剂,化学反应生成 妥卡尼
参考文献:Primary Aminoacylanilides,Methods Of Making The Same And Use As
标题:Primary Aminoacylanilides,Methods Of Making The Same And Use As
摘要:主要氨基酰基苯胺的结构式为##str1##其中r.Sub.1从氢,甲基,乙基和丙基中选择,R.Sub.2从甲基,乙基,氯,甲氧基和乙氧基中选择,R.Sub.3从氢和甲基中选择,R.Sub.4从氢,甲基和c.Sub.1-C.Sub.4烷氧基中选择,R.Sub.6从甲基,乙基,氯,甲氧基和乙氧基中选择,R.Sub.7为氢,甲基或乙基,R.Sub.8为氢,R.Sub.9为氢,甲基或乙基,R.Sub.10为氢,N为0或1,具体规定如下:(A)当n为0时,R.Sub.8也可以是甲基;(B)当n为1且r.Sub.7为氢,R.Sub.9为氢或甲基时,R.Sub.10也可以是甲基;(C)当r.Sub.1为氢,R.Sub.2为甲基,R.Sub.3为氢,R.Sub.6为甲基,R.Sub.7为氢,R.Sub.8为氢,N为0时,R.Sub.4只能是乙氧基或丙氧基;(D)当r.Sub.1为氢,R.Sub.2为甲基,R.Sub.3,R.Sub.4,R.Sub.7和r.Sub.8为氢,N为0时,R.Sub.6只能是甲氧基,乙氧基或乙基;以及其治疗上可接受的盐.已发现这类化合物在口服给药时,特别是作为长效心脏抗心律失常药物,具有非常好的疗效.

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-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-9964032-A1
优先权日:1998-06-08
标题 :Combinatorial synthesis of multibinding libraries
发明人：CHRISTENSEN BURTON G; GRIFFIN JOHN H; JENKINS THOMAS E; JUDICE J KEVIN
权利人:ADVANCED MEDICINE INC; CHRISTENSEN BURTON G; GRIFFIN JOHN H; JENKINS THOMAS E; JUDICE J KEVIN
摘要:Disclosed are methods for synthesizing large collections of diverse multimeric compounds as well as iterative processes for evaluating key molecular constraints imparting multibinding properties to multimeric compounds. Also disclosed are libraries of multimeric compounds which can be evaluated for imparting multibinding properties.

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:US-9757463-B2
优先权日:2012-06-15
标题 :Linear polyester and semi-linear glycidol polymer systems: formulation and synthesis of novel monomers and macromolecular structures
发明人：HARTH EVA M; BEEZER DAIN B; LI GUANGZHAO; SPEARS BENJAMIN R; STEVENS DAVID M
权利人:UNIV VANDERBILT
摘要:Disclosed herein are glycidol-based polymers, nanoparticles, and methods related thereto useful for drug delivery. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.