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-9700244-A1 优先权日:1995-06-19 标题 :Process for parallel synthesis of a non-peptide library 发明人:FRITZ JAMES E; KALDOR STEPHEN W 权利人:LILLY CO ELI; FRITZ JAMES E; KALDOR STEPHEN W 摘要:A process for the sequential preparation of a library of compounds having pharmaceutical usage. The process involves the sequential mixing of solution phase reagents, followed by scavenging of excess unreacted reagents with solid phase scavenging agents. The process is highly iterative and applicable for producing various ureas, thiureas, amides, carbonates and tertiary amines.
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
专利号:US-8372971-B2 优先权日:2004-08-25 标 题:Heterocyclic compounds and methods of use 发明人:WRASIDLO WOLFGANG; DNEPROVSKAIA ELENA 权利人:TARGEGEN INC; WRASIDLO WOLFGANG; DNEPROVSKAIA ELENA 摘要:Heterocyclic compounds derived from benzotriazine, triazines, triazoles and oxadiazoles are disclosed. The methods of synthesis and of use of such heterocyclic compounds are also provided.
专利号:WO-9700872-A1 优先权日:1995-06-23 标题 :1,3,8-triaza- and 3,8-diaza-1-oxaspiro(4,5)decane derivatives 发明人:BERGER JACOB; CARTER DAVID SCOTT; FLIPPIN LEE ALLEN; WEINHARDT KLAUS KURT 权利人:HOFFMANN LA ROCHE 摘要:Heterocyclic compounds of Formula (I) in which n is 2, 3, 4, 5 or 6; t is 1, 2, 3 or 4; u is 0 or 1 (provided that t is not 1 when u is 0); X is O or N(R4), in which R4 is hydro, (C¿1-4?)alkyl, or aryl; Y and Z are independently C(O), C(S) or CH2 (provided that Y and Z are not both CH2); R?1, R2, and R3¿ are as defined in the specification; and their pharmaceutically acceptable salts and N-oxides, formulations containing them, their uses as therapeutic agents, and their synthesis. The compounds of this invention are selective 5-HT¿2?C receptor antagonists.
摘要:Koutentis, P. A.; Ioannidou, H. A., Science of Synthesis Knowledge Updates, (2010) 1, 305. 摘要:Götzinger, A. C.; Müller, T. J. J., Science of Synthesis Knowledge Updates, (2017) 3, 36. 摘要:Aitken, R. A., Science of Synthesis Knowledge Updates, (2018) 3, 355.