专利号:US-4822903-A 优先权日:1981-05-15 标题:Fluorinated silica catalyst and preparation of aromatic/aliphatic nitriles in the presence thereof 发明人:JACQUES ROLAND; REPPELIN MICHEL; SEIGNEURIN LAURENT 权利人:RHONE POULENC SPEC CHIM 摘要:An improved fluorinated siliceous catalyst, well adapted for the catalytic synthesis of aromatic/aliphatic nitriles from their corresponding formamides, formanilides or amides, is comprised of a plurality of silica particulates, the specific surface of which ranging from about 200 to about 300 m 2 /g, having a total pore volume ranging from about 1 to about 1.5 cm 3 /g, with an average pore diameter ranging from about 100 to about 200 â„«, having an exchange pH of less than about 3, and with the fluorine content thereof bonded to the silica, expressed in F 31 , ranging from about 0.05 to about 2% by weight based upon the silica, and the sodium content thereof, expressed as Na 2 O, being less than about 1% by weight, also based upon the silica.
专利号:US-8003785-B2 优先权日:2008-06-18 标 题 :Halo-substituted pyrimidodiazepines 发明人:CAI JIANPING; CHEN SHAOQING; CHU XIN-JIE; LUK KIN-CHUN; MISCHKE STEVEN GREGORY; SUN HONGMAO; WOVKULICH PETER MICHAEL 权利人:TAKEDA PHARMACEUTICAL 摘要:The present invention provides PLK1 inhibitor compounds of formula I: n nuseful in the treatment or control of cell proliferative disorders, particularly oncological disorders. These compounds and formulations containing such compounds may be useful in the treatment or control of solid tumors, such as, for example, breast, colon, lung and prostate tumors and other oncological diseases such as non-Hodgkin's lymphomas. Also provided are intermediate compounds useful in the synthesis of compounds of formula I.
专利号:US-7579356-B2 优先权日:2005-05-04 标 题:Thia-tetraazaacenaphthylene kinase inhibitors 发明人:BATTISTA KATHLEEN A; BIGNAN GILLES C; CONNOLLY PETER J; HAYDEN STUART; JOHNSON SIGMOND G; LIN RONGHUI; PANDEY NIRANJAN B; POWELL MARK T 权利人:JANSSEN PHARMACEUTICA NV 摘要:The present invention is directed to novel thia-tetraazaacenaphthylene compounds of Formula (I): n nand pharmaceutically acceptable forms thereof and their synthesis and use as inhibitors of ATP-protein kinase interactions.
专利号:US-10017481-B2 优先权日:2012-03-17 标 题 :Conformationally constrained, fully synthetic macrocyclic compounds 发明人:OBRECHT DANIEL; ERMERT PHILIPP; OUMOUCH SAID; PIETTRE ARNAUD; GOSALBES JEAN-FRANÇOIS; THOMMEN MARC 权利人:POLYPHOR AG 摘要:The conformationally restricted, spatially defined macrocyclic ring system of formula (I) is constituted by three distinct molecular parts: Template A, conformation Modulator B and Bridge C. Macrocycles described by this ring system I are readily manufactured by parallel synthesis or combinatorial chemistry in solution or on solid phase. They are designed to interact with a variety of specific biological target classes, examples being agonistic or antagonistic activity on G-protein coupled receptors (GPCRs), inhibitory activity on enzymes or antimicrobial activity. In particular, these macrocycles show inhibitory activity on endothelin converting enzyme of subtype 1 (ECE-1) and/or the cysteine protease cathepsin S (CatS), and/or act as antagonists of the oxytocin (OT) receptor, thyrotropin-releasing hormone (TRH) receptor and/or leukotriene B4 (LTB4) receptor, and/or as agonists of the bombesin 3 (BB3) receptor, and/or show antimicrobial activity against at least one bacterial strain. Thus they are showing great potential as medicaments for a variety of diseases.
专利号:US-8513241-B2 优先权日:2008-03-28 标题 :3,4-dihydro-2H-pyrazino[1,2-A]indol-1-one derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them 发明人:CERVI GIOVANNI; D ANELLO MATTEO; PAPEO GIANLUCA MARIANO ENRICO; SALOM BARBARA 权利人:CERVI GIOVANNI; D ANELLO MATTEO; PAPEO GIANLUCA MARIANO ENRICO; SALOM BARBARA; NERVIANO MEDICAL SCIENCES SRL 摘要:Compounds which are 3,4-dihydro-2H-pyrazino[1,2-a]indol-1-one derivatives or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.
专利号:CN-109369555-A 优先权日:2018-11-29 标题 :A kind of method of microwave radiation benzamide compound synthesis benzoxazoles in water phase
[参考文献]: Mehrdad Pourayoubi, Et Al. N-(3-Fluoro-Benzo-Yl)-N',N''-Bis-(4-Methyl-Phen-Yl)Phospho-Ric Triamide. Acta Crystallogr Sect E Struct Rep Online. 2011 Nov;67(Pt 11):O3034.
合成参考文献
参考文献:10.1055/s-0035-1560876 摘要:Palladium/Carbon-Catalyzed Aminocarbonylation of Aryl Iodides. Synfacts. 2015 Nov 17;11(12):1336. doi: 10.1055/s-0035-1560876. 参考文献:10.1055/s-0033-1340162 摘要:Bhanage B, Gadge S. A Phosphine-Free Approach to Primary Amides by Palladium-Catalyzed Aminocarbonylation of Aryl and Heteroaryl Iodides Using Methoxylamine Hydrochloride as an Ammonia Equivalent. Synlett. 2013 Nov 05;25(01):85–8. doi: 10.1055/s-0033-1340162.