CAS: 493-78-7; N,N-Dimethyl-N'-Phenyl-N'-(Thiophen-2-Ylmethyl)Ethane-1,2-Diamine

📜N,N-二甲基-N'-苯基乙二胺置于sodium Amide,甲苯体系中,化学反应生成 美沙芬林
参考文献:具有抗组胺活性的2-噻吩取代的二胺.
标题:具有抗组胺活性的2-噻吩取代的二胺.
摘要:
DOI:10.1021/ja01186A023

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:US-9410004-B2
优先权日:2008-05-21
标 题 :Aromatic polyethersulfone microparticles having narrow particle diameter distribution index
发明人：ASANO ITARU; ECHIGO YUJI; TAKEZAKI HIROSHI
权利人:TORAY INDUSTRIES
摘要:A fine polymer particle production method includes producing an emulsion in a liquid prepared by dissolving and mixing a polymer A and a polymer B in organic solvents in which a solution phase composed primarily of the polymer A and a solution phase composed primarily of the polymer B are formed as separate phases, and bringing it into contact with a poor solvent for the polymer A to precipitate the polymer A. This method serves for easy synthesis of fine polymer particles with a narrow particle size distribution and the method can be effectively applied to production of highly heat-resistant polymers that have been difficult to produce with the conventional methods.

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: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