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-9908846-B2 优先权日:2014-02-21 标题:Composition, synthesis, and use of new arylsulfonyl isonitriles 发明人:FLEMING FRASER FERGUSSON; LUJAN MONTELONGO JESUS ARMANDO 权利人:DUQUESNE UNIV OF THE HOLY GHOST; UNIV HOLY GHOST DUQUESNE 摘要:This invention relates to novel isonitriles, including arylsulfonyl isonitriles, and methods for their synthesis. The isonitriles include a conjugated ring system. The structure is designed with the flexibility to have multiple substitution patterns. The isonitriles may be used in applications including, but not limited to, pharmaceutical compositions.
专利号:US-2015239833-A1 优先权日:2014-02-21 标题:Composition, synthesis, and use of new arylsulfonyl isonitriles
专利号:CN-116768814-A 优先权日:2023-06-30 标 题 :A kind of synthesis method of 4-sulfonyl-2,5-bis(trifluoromethyl)oxazole compound
专利号:CN-110183379-B 优先权日:2019-06-22 标 题 :Synthesis method and application of copper-catalyzed one-pot method for preparing C-4-sulfonyl substituted isoquinolone compounds