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:RU-2035452-C1 优先权日:1985-12-20 标 题 :Method of n-phenylpyrazole synthesis
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
参考标题:Unconventional Stereoselective One-Pot Synthesis Of Knoevenagel-Type Indoles Via In Situ Condensation Of Iminium Salts With Active Methylene Reagents 作者:Angelo Ranise,Francesco Lucchesini,Matteo Caviglia,Silvana Alfei,Andrea Spallarossa,Chiara Caneva |发布日期:2013.12 摘要:Knoevenagel-Type Indoles Is Described. The Method Is Based On The In Situ Reaction Of Indole Iminium Salts (Four Of Them Are Fully Characterized) With Acyclic Symmetrical And Unsymmetrical Active Methylene Reagents In The Presence Of Triethylamine. In General, The Overall Yields Are Moderate To Good. Some Of Relevant Reaction Parameters And Steric Effects Affecting Stereoselectivity Are Discussed.