CAS: 21512-15-2; Citenazone

📜,5-氰基-2-噻吩甲醛,,,,5-Cyano-Thiophen-2-Aldehyde-S-Allyl-Isothiosemicarbazone-Hydrobromide,,,以 Anhydrous Ethylene Glycol Dimethyl Ether 用作溶剂,以the Above-Mentioned Compounds Were Also Obtained By The Reaction Of 5-Cyano-Thiophen-2-Aldehyde-Thiosemicarbazone With The Corresponding Alkyl-Or Aralkyl-Halides In Ethylene-Glycol-Monomethyl Ether At 50°-60oc.的收率获得氰噻腙
参考文献:5-Cyano-Thiophen-2-Aldehyde-Isothiosemicarbazones And Process For
标题:5-Cyano-Thiophen-2-Aldehyde-Isothiosemicarbazones And Process For
摘要:本发明涉及一种制备新型5-氰基噻吩-2-甲醛异硫脲半胱氨酸酮类化合物的方法.这些化合物对病毒具有活性,因此适用于预防和治疗人类和动物相应感染.

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: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