CAS: 1943-82-4; 2-Phenylethyl Isocyanate

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2-(Phenethylamino)-2-Oxoacetic Acid置于collidine体系中,用 乙腈 用作溶剂,化学反应生成2-苯乙基异氰酸酯
参考文献:支持无电解质的草酸阳极氧化为异氰酸酯:一种获得尿素,氨基甲酸酯和硫代氨基甲酸酯的便捷方法
标题:支持无电解质的草酸阳极氧化为异氰酸酯:一种获得尿素,氨基甲酸酯和硫代氨基甲酸酯的便捷方法
摘要:我们报告了一种新的电化学无负载电解质方法,用于通过草酸氧化合成尿素,氨基甲酸酯和硫代氨基甲酸酯.这种简单,实用且无光气的路线包括在有机碱存在下通过草酸的阳极脱羧原位生成异氰酸酯中间体,然后一锅加入合适的亲核试剂以提供相应的尿素,氨基甲酸酯和硫代氨基甲酸酯.此程序适用于不同的胺,醇和硫醇.此外,当使用单程连续电化学流动条件并且该反应在碳石墨 C Gr /c Gr 在流动池中,可以在 6 分钟的停留时间内以高产率获得尿素化合物,解锁在批量条件下无法访问的底物,同时易于扩展.
Doi:10.1021/acs.Oprd.1C00112

专利信息

专利号:US-7138526-B1
优先权日:1999-06-15
标 题 :Solid phase synthesis of n,n-disubstituted diazacycloalkylcarboxy derivatives
发明人：HERPIN TIMOTHY F; MORTON GEORGE C; SALVINO JOSEPH M
权利人:AVENTIS PHARMA INC
摘要:A method for the solid phase synthesis of N,N-disubstituted diazacycloalkylcarboxy derivatives of general formula (I) and (II) is claimed. Examples include piperazine-2-carboxamide. The method is applicable to the synthesis or large combinatorial libraries

专利号:US-4108870-A
优先权日:1977-06-06
标 题:Stereocontrolled synthesis of α-multistriatin
发明人：FRIED JOSEF; ELLIOTT WILLIAM J
权利人:UNIV CHICAGO
摘要:A practical stereocontrolled synthesis of a mixture containing a major amount of α-multistriatin and a minor amount of γ-multistriatin in an overall yield of about 73% from cis-2-butene-1,4-diol is provided. α-Multistriatin is one of the three essential components of the aggregation pheromone of the European elm bark beetle.

专利号:US-2007082943-A1
优先权日:2005-04-01
标 题:Process for preparation of substantially pure glimepiride
发明人：KADAM SURESH M; TARUR VENKATASUBRAMANIAN R; NAIK SANJAY J; GAVHANE SACHIN B
权利人:KADAM SURESH M; TARUR VENKATASUBRAMANIAN R; NAIK SANJAY J; GAVHANE SACHIN B
摘要:The present invention discloses a novel process for purification of trans-4-methyl cyclohexylamine HCl and 4[-2-(3-Ethyl-4-methyl-2-carbonyl pyrrolidine amido) ethyl] benzene sulfonamide used in the synthesis of 3-Ethyl-2,5-dihydro-4-methyl-N-[2-[4-[[[[(trans-4-methyl cyclohexyl)amino]carbonyl]amino]sulfonyl]phenyl]ethyl]-2-oxo-1H-pyrrole-1-carboxamide (I), popularly known as Glimepiride. The present invention also discloses a novel purification of Glimepiride usingS methanolic ammonia and glacial acetic acid to obtain highly pure Glimepiride Form I (I) having the undesired cis isomer below 0.15%. Glimepiride (I) is useful in the treatment of diabetes mellitus.

专利号:US-6432933-B1
优先权日:1997-07-07
标 题 :Glycol and hydroxyphosphonate peptidomimetics as inhibitors of aspartyl proteases
发明人：CARROLL CAROLYN DIIANNI; DOLLE III ROLAND ELLWOOD; SHIMSHOCK YVONNE CLASS; HERPIN TIMOTHEE FELIX
权利人:PHARMACOPEIA INC
摘要:Compounds of Formula I n are disclosed as inhibitors having activity against the aspartyl proteases, plasmepsin and cathepsin D. The compounds are therefore useful for treatment of diseases such as malaria and Alzheimer's disease. In preferred compounds of Formula I, Y is an dialkoxyphosphonate, or α-hydroxyamide group and Z is an acyl or α-ketocarbamate functionality. Intermediates in the solid phase synthesis of compounds of Formula I, in which compounds are attached to a solid support, are also disclosed.

专利号:WO-9700244-A1
优先权日:1995-06-19
标题 :Process for parallel synthesis of a non-peptide library
发明人：FRITZ JAMES E; KALDOR STEPHEN W
权利人:LILLY CO ELI; FRITZ JAMES E; KALDOR STEPHEN W
摘要:A process for the sequential preparation of a library of compounds having pharmaceutical usage. The process involves the sequential mixing of solution phase reagents, followed by scavenging of excess unreacted reagents with solid phase scavenging agents. The process is highly iterative and applicable for producing various ureas, thiureas, amides, carbonates and tertiary amines.

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.