3-氨基苯酚置于palladium 10% On Activated Carbon,氢气体系中,用 甲醇 作为反应溶剂,60.0 °C,101.33 Kpa 条件下,反应 14.0H,以94%的收率获得产物3-氨基-2-环己烯-1-酮 参考文献:A Practical And One-Pot Procedure For The Synthesis Of 3-Amino-2-Cyclohexen-1-One From 3-Aminophenol 标题:A Practical And One-Pot Procedure For The Synthesis Of 3-Amino-2-Cyclohexen-1-One From 3-Aminophenol 摘要:A Simple,Totally Catalytic,And Environmentally Benign Process For The Synthesis Of 3-Amino-2-Cyclohexen-1-One Using 10% Pd/c-Catalyzed Hydrogenation Has Been Developed. DOI:10.1021/op0497761
专利号:US-2007197797-A1 优先权日:2005-12-30 标 题 :Compounds and methods for carbazole synthesis 发明人:HARRINGTON PETER J 权利人:HARRINGTON PETER J 摘要:Compounds having bi-cyclic structure comprising a partially unsaturated 6-carbon first cyclic moiety interconnected to a 6-carbon second cyclic moiety second via a divalent linking moiety are provided. The compounds can be used as intermediates compounds in methods for the synthesis of carbazoles and derviatives thereof, including carvedilol, and tricyclic alkylhydroxamates, which do not require Fischer indole synthetic steps. Methods of preparing the compounds having bi-cyclic structures are also provided.
专利号:US-5767131-A 优先权日:1993-04-05 标 题 :Dihydropyridines and new uses thereof 发明人:GLUCHOWSKI CHARLES; WETZEL JOHN M; CHIU GEORGE; MARZABADI MOHAMMED R; WONG WAI C; NAGARATHNAM DHANAPALAN 权利人:SYNAPTIC PHARMA CORP 摘要:The invention provides a method of treating benign prostatic hyperplasia in a subject which comprises administering to the subject a therapeutically effective amount of a compound having the structure: ##STR1## wherein Y is --(CH 2 ) n --, where n is 1, 2, 3, 4 or 5; --(CH 2 ) h --O--(CH 2 ) k --, where h and k are independently the same or different and are 2, 3 or 4; --(CH 2 ) h --CHâ•?CH--(CH 2 ) k --; or --(CH 2 ) h --C.tbd.C--(CH 2 ) k --, where h and k are independently the same or different and are 1, 2, 3 or 4; wherein Z is O, NH, or CH 2 ; wherein R 1 is a linear or branched chain alkyl, alkoxyalkyl or arylalkyl group; wherein R 2 and R 4 are independently the same or different and are H, or a linear or branched chain alkyl group; wherein R 3 is H, a linear or branched chain alkyl, alkoxy, alkoxyalkyl or acyl group; and wherein R 5 and R 6 are independently the same or different and are H, OH, Cl, Br, F, NO 2 , CN, CF 3 , or NH 2 , or a linear or branched chain alkyl, alkoxy, alkoxycarbonyl, acyl, alkylsulfoxide, alkylsulfone, or mono- or dialkylamino group. Other active compounds containing one, two or three rings are also disclosed as well as pharmaceutical compositions prepared therefrom and methods of use in the treatment of BPH, inhibition of cholesterol synthesis, and reduction of intraocular pressue.
专利号:US-6608086-B2 优先权日:1993-04-05 标 题:Dihydropyridines and new uses thereof 发明人:GLUCHOWSKI CHARLES; WETZEL JOHN M; CHIU GEORGE; MARZABADI MOHAMMED R; WONG WAI C; NAGARATHNAM DHANAPALAN 权利人:SYNAPTIC PHARMA CORP 摘要:This invention provides dihydropyridines useful for treatment of prostatic hyperplasia, inhibition of cholesterol synthesis, and/or reduction of intraocular pressure.
[参考文献]: Atul R Gholap, Et Al. Synthesis And Evaluation Of Antifungal Properties Of A Series Of The Novel 2-Amino-5-Oxo-4-Phenyl-5,6,7,8-Tetrahydroquinoline-3-Carbonitrile And Its Analogues. Bioorg Med Chem. 2007 Nov 1;15(21):6705-15.
合成参考文献
摘要:Spitzner, D., Science of Synthesis Knowledge Updates, (2016) 1, 99.