CAS: 35303-76-5; 4-(2-Aminoethyl)Benzenesulfonamide

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CAS号3665-08-5 Benzenesulfonam... | CAS号41472-49-5 N-[2-[4-(氨基磺酰基)... | CAS号877-95-2 N-(2-苯乙基)乙酰胺 | CAS号35450-53-4 p-(2-acetamidoe... | CAS号41472-49-5 N-[2-[4-(氨基磺酰基)... | CAS号10079-93-3 1-phenyl-3-[2-(... | CAS号345970-48-1 4-[2-[(4-aminop... | CAS号16673-34-0 4-[2-(5-氯-2-甲氧基... | CAS号59477-42-8 4-chloro-N-[2-(... | CAS号54160-75-7 1-methyl-1-phen...

4-(氰基甲基)苯磺酰胺置于镍 Sodium Methylate体系中,用 甲醇 作为反应溶剂,以86%的收率获得产物4-(2-氨乙基)苯磺酰胺
参考文献:氰基磺酰胺的电化学还原新合成马芬尼德和其他氨基磺酰胺
标题:氰基磺酰胺的电化学还原新合成马芬尼德和其他氨基磺酰胺
摘要:脂肪族和芳香族氨基磺酰胺类化合物(如马芬尼(1A))是通过在含ni阴极,Pt阳极和阮内ni作为催化剂的未分隔电池中将相应的腈直接电化学加氢而以高收率(80-86%)合成的(表1).该反应可以在不通过原位产生h 2的外部供应加压气体的情况下进行.略微升高温度(45°)和低电流密度(10 Ma / Cm 2)是这种类型的电化学腈加氢的有利条件.我们的合成规程不需要高压设备或化学危害,在环境方面非常友好,比传统方法更经济.吸附的h的浓度.通过调节电势可以轻松控制催化剂表面的自由基,这可以提高产品的选择性,同时降低爆炸和着火的风险.
DOI:10.1002/hlca.200690123

专利信息

专利号:US-5877278-A
优先权日:1992-09-24
标题:Synthesis of N-substituted oligomers
发明人：ZUCKERMANN RONALD N; GOFF DANE A; NG SIMON; SPEAR KERRY; SCOTT BARBARA O; SIGMUND AARON C; GOLDSMITH RICHARD A; MARLOWE CHARLES K; PEI YAZHONG; RICHTER LUTZ; SIMON REYNA
权利人:CHIRON CORP
摘要:A solid-phase method for the synthesis of N-substituted oligomers, such as poly (N-substituted glycines) (referred to herein as poly NSGs) is used to obtain oligomers, such as poly NSGs of potential therapeutic interest which poly NSGs can have a wide variety of side-chain substituents. Each N-substituted glycine monomer is assembled from two 'sub-monomers' directly on the solid support. Each cycle of monomer addition consists of two steps: (1) acylation of a secondary amine bound to the support with an acylating agent comprising a leaving group capable of nucleophilic displacement by -NH2, such as a haloacetic acid, and (2) introduction of the side-chain by nucleophilic displacement of the leaving group, such as halogen (as a solid support-bound alpha -haloacetamide) with a sufficient amount of a second sub-monomer comprising an -NH2 group, such as a primary amine, alkoxyamine, semicarbazide, acyl hydrazide, carbazate or the like. Repetition of the two step cycle of acylation and displacement gives the desired oligomers. The efficient synthesis of a wide variety of oligomeric NSGs using automated synthesis technology of the present method makes these oligomers attractive candidates for the generation and rapid screening of diverse peptidomimetic libraries. The oligomers of the invention, such as N-substituted glycines (i.e. poly NSGs) disclosed here provide a new class of peptide-like compounds not found in nature, but which are synthetically accessible and have been shown to possess significant biological activity and proteolytic stability. Combinatorial libraries of cyclic compounds are disclosed wherein the cyclic compounds are comprised of at least one ring structure derived from cyclization of a peptoid backbone. The diversity of product compounds is generated by the sequential addition of substituted submonomers. The combinatorial library includes 10 or more, preferably 100 or more, and more preferably 1,000 or more distinct and different compounds. The library includes each of the product compounds in retrievable and analyzable amounts and preferably includes at least one biologically active compound. Methods of synthesizing the combinatorial libraries and assay devices produced using the libraries are disclosed as is methodology for screening for and obtaining biologically active cyclic organic compounds.

专利号:WO-0140193-A1
优先权日:1999-12-03
标题:Method for the synthesis of pyrazolines
发明人：BOLDI ARMEN M
权利人:CHEMRX ADVANCED TECHNOLOGIES I; BOLDI ARMEN M
摘要:The present invention provides a method for the synthesis of compounds of Formula (I). Also claimed are novel intermediates and their methods of synthesis.

专利号:US-2002103381-A1
优先权日:2000-11-30
标 题 :Method for the synthesis of pyrazolines
发明人：BOLDI ARMEN M
摘要:The present invention provides a method for the synthesis of compounds of Formula I: n n n Also claimed are novel intermediates and their methods of synthesis.

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-7109377-B2
优先权日:1996-10-16
标 题:Synthesis of combinatorial libraries of compounds reminiscent of natural products
发明人：SCHREIBER STUART L; SHAIR MATTHEW D; TAN DEREK S; FOLEY MICHAEL A; STOCKWELL BRENT R
权利人:HARVARD COLLEGE
摘要:The present invention provides complex compounds reminiscent of natural products and libraries thereof, as well as methods for their production. The inventive compounds and libraries of compounds are reminiscent of natural products in that they contain one or more stereocenters, and a high density and diversity of functionality. In general, the inventive libraries are synthesized from diversifiable scaffold structures, which are synthesized from readily available or easily synthesizable template structures. In certain embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from a shikimic acid based epoxyol template. In other embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from the pyridine-based template isonicotinamide. The present invention also provides a novel ortho-nitrobenzyl photolinker and a method for its synthesis. Furthermore, the present invention provides methods and kits for determining one or more biological activities of members of the inventive libraries. Additionally, the present invention provides pharmaceutical compositions containing one or more library members.

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.