CAS: 91-79-2; N,N-Dimethyl-N'-[2]Pyridyl-N'-[3]Thienylmethyl-Ethylenediamine

上下游产品

3-Bromomethylthiophene N,N-dimethyl-N'-(pyridine-2-yl)ethane-1,2-diamine diethyl ether 2-bromothiophene-4-carboxylic acid

📜5-Bromo-Thiophene-3-Carboxylic Acid-[(2-Dimethylamino-Ethyl)-[2]Pyridyl-Amide]置于lithium Aluminium Tetrahydride,乙醚体系中,化学反应生成 西尼二胺
参考文献:3-Substituted Thiophenes. Vi. Substitution Reactions Of 3-Thenoic Acid
标题:3-Substituted Thiophenes. Vi. Substitution Reactions Of 3-Thenoic Acid
摘要:
DOI:10.1021/ja01638A041

专利信息

专利号:WO-9837078-A1
优先权日:1997-02-20
标题 :Solid phase and combinatorial synthesis of substituted thiophenes and of arrays of substituted thiophenes
发明人：DOERWALD FLORENCIO ZARAGOZA
权利人:NOVO NORDISK AS
摘要:A solid phase method for the synthesis of a plurality of differently substituted thiophenes with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The thiophenes are prepared by reaction of a substrate-bound primary or secondary amine with a thiophosgene equivalent and reaction of the resulting intermediate with an acceptor-substituted acetonitrile in the presence of a base. Alkylation with an appropriate alkyl halide, followed by Thorpe-Ziegler-cyclization yields differently substituted, support-bound 3-aminothiophenes. These may be screened on the substrate or cleaved from the substrate and then screened in solution. Alternatively, the resin-bound 3-amino thiophenes or the synthetic intermediates can be subjected to further synthetic transformations (N-acylation, reduction) on the support, which permits the preparation of further therapeutically interesting compounds. The efficient synthesis of a wide variety of thiophenes using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse thiophene-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.

专利号:US-6136984-A
优先权日:1996-04-22
标 题 :Solid phase and combinatorial synthesis of substituted thiophenes and of arrays of substituted thiophenes
发明人：DOERWALD FLORENCIO ZARAGOZA
权利人:NOVO NORDISK AS
摘要:A solid phase method for the synthesis of a plurality of differently substituted thiophenes with a wide variety of side-chain substituents as compounds of potential therapeutic interest is disclosed. The thiophenes are prepared by acylation of a substrate-bound primary or secondary amine with cyanoacetic acid and reaction of the resulting cyanoacetamide with an isothiocyanate in the presence of a base. Alkylation with an appropriate alkyl halide, followed by Thorpe-Ziegier-cyclization yields differently substituted, support-bound 3-aminothiophenes. These may be screened on the substrate or cleaved from the substrate and then screened in solution. Alternatively, the resin-bound 3-amino thiophenes or the synthetic intermediates can be subjected to further synthetic transformations (N-acylation, reduction) on the support, which permits the preparation of further therapeutically interesting compounds. The efficient synthesis of a wide variety of thiophenes using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse thiophene-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.

专利号:EP-4198027-A1
优先权日:2021-12-14
标题:Sustainable process for the synthesis of molecules with antihistamine activity in unconventional biodegradable solvents (deep eutectic solvents)
发明人：QUIVELLI ANDREA FRANCESCA; CAPRIATI VITO; PERNA FILIPPO MARIA; VITALE PAOLA; ROSSI FEDERICO VITTORIO; GARCÃ A - Ã LVAREZ JOAQUÃ N
权利人:UNIV DEGLI STUDI DI BARI; UNIV OVIEDO
摘要:The present invention relates to a sustainable synthetic process for obtaining ethylenediamines molecules with antihistamine activity whose production costs are considerably reduced by employing unconventional biodegradable solvents, such as the Deep Eutectic Solvents, with considerable advantages from a point of view both of the environmental and economic impact.

专利号:WO-9740034-A1
优先权日:1996-04-22
标题:Solid phase and combinatorial synthesis of substituted thiophenes and of arrays of substituted thiophenes

专利号:JP-2000508664-A
优先权日:1996-04-22
标题:Solid-phase and combinatorial synthesis of substituted thiophenes and arrays of substituted thiophenes

专利号:EP-1021435-A1
优先权日:1996-04-22
标题:Solid phase and combinatorial synthesis of substituted thiophenes and of arrays of substituted thiophenes