环丁基甲酰氯置于乙醚,Sodium体系中,化学反应生成 环丁基甲醇 参考文献:Perkin Junior,W. H.,Journal Of The Chemical Society,1901,Vol. 79,P. 329 标题:Perkin Junior,W. H.,Journal Of The Chemical Society,1901,Vol. 79,P. 329
专利号:US-7598399-B2 优先权日:2005-11-30 标 题 :Methods for synthesis of 3-amino-1-arylpropyl indoles 发明人:CONNOLLY TERRENCE JOSEPH; FARRELL ROBERT P; HUMPHREYS ERIC ROY; LYNCH STEPHEN M; SARMA KESHAB 权利人:ROCHE PALO ALTO LLC 摘要:A method comprising:n hydrogenating an indole propionamide compound of formula h nn nwith vitride, to form an aminopropyl indole compound of formula in n nwherein m, Ar, R 1 and R 2 are as defined herein. The compounds prepared by the method of the invention are useful as monoamine reuptake inhibitors useful for treatment of CNS indications.
专利号:US-5637757-A 优先权日:1995-04-11 标 题 :One-pot synthesis of ring-brominated benzoate compounds 发明人:HILL JOHN E; FAVSTRITSKY NICOLAI A; MAMUZIC RASTKO I; BHATTACHARYA BHABATOSH 权利人:GREAT LAKES CHEMICAL CORP 摘要:A method of preparing tetrabromobenzoate compounds from tetrabromophthalic anhydride by reacting tetrabromophthalic anhydride with alcohol in the presence of a decarboxylation catalyst. The reaction may be carried out in an excess of alcohol, or with a near stoichiometric amount of alcohol by performing the reaction in an inert solvent.
专利号:US-2004053999-A1 优先权日:1997-09-17 标题 :Novel compounds and methods for synthesis and therapy 发明人:BISCHOFBERGER NORBERT W; DAHL TERRENCE C; HITCHCOCK MICHAEL J M; KIM CHOUNG U; LEW WILLARD; LIU HONGTAO; MILLS ROGER G; WILLIAMS MATTHEW A 摘要:Novel compounds are described. The compounds generally comprise an acidic group, a basic group, a substituted amino or N-acyl and a group having an optionally hydroxylated alkane moiety. Pharmaceutical compositions comprising the inhibitors of the invention are also described. Methods of inhibiting neuraminidase in samples suspected of containing neuraminidase are also described. Antigenic materials, polymers, antibodies, conjugates of the compounds of the invention with labels, and assay methods for detecting neuraminidase activity are also described.
专利号:US-6225341-B1 优先权日:1995-02-27 标 题:Compounds and methods for synthesis and therapy 发明人:BISCHOFBERGER NORBERT W; KIM CHOUNG U; LEW WILLARD; LIU HONGTAO; WILLIAMS MATTHEW A 权利人:GILEAD SCIENCES INC 摘要:Novel compounds are described. The compounds generally comprise an acidic group, a basic group, a substituted amino or N-acyl and a group having an optionally hydroxylated alkane moiety. Pharmaceutical compositions comprising the inhibitors of the invention are also described. Methods of inhibiting neuraminidase in samples suspected of containing neuraminidase are also described. Antigenic materials, polymers, antibodies, conjugates of the compounds of the invention with labels, and assay methods for detecting neuraminidase activity are also described.
专利号:WO-9419023-A1 优先权日:1993-02-19 标 题:Cyclobutyl antisense oligonucleotides, methods of making and use thereof 发明人:COOK PHILLIP DAN; BASCHANG GERHARD 权利人:ISIS PHARMACEUTICALS INC 摘要:Oligonucleotide surrogates comprising a plurality of cyclobutyl moieties covalently joined by linking moieties are prepared and used as antisense diagnostics, therapeutics and research reagents. Methods of synthesis and use of both the oligonucleotide surrogates and intermediates thereof are disclosed.
专利号:WO-2010115869-A1 优先权日:2009-04-03 标 题 :Propofol phosphonyl derivatives, synthesis, and use in long acting formulations 发明人:GONNISSEN YVES RENE JOHANNA PAUL 权利人:SEPS PHARMA N V; GONNISSEN YVES RENE JOHANNA PAUL 摘要:This invention relates to compounds represented by the structural formula (I), and the salts and stereoisomers thereof, wherein: - L is a linker selected from the group consisting of -(CH 2 ) P -O-, a single bond, formula (IA), -(CH 2 ) 1-8 -O-X(O)-, and - p is an integer from 1 to 8, - each R 3 and each R 4 is independently selected from the group consisting of C 1-20 alkyl, C 3-12 alkyl, C 3-12 cycloalkyl-C 1-4 alkyl, saturated heterocyclyl and saturated heterocyclyl-C 1-4 alkyl, and - X and Y are each independently C or S(O), - Z is selected from the group consisting of O, S(O) and NR 5 , - W is selected from the group consisting of halogen, OH, S(O)H and O - M + wherein M + is a monovalent cation; and - R 5 is selected from the group consisting of hydrogen and C 1-10 alkyl. These compounds are useful pharmaceutical agents with improved oral bioavailability.
[参考文献]: Ken-Ichi Takao, Et Al. Total Synthesis Of (-)-Pestalotiopsin A. Angew Chem Int Ed Engl. 2008;47(18):3426-9.
合成参考文献
摘要:Wu, X.-F., Science of Synthesis Knowledge Updates, (2014) 1, 328. 摘要:Götzinger, A. C.; Müller, T. J. J., Science of Synthesis Knowledge Updates, (2017) 3, 172. 摘要:Casano, G.; Ouari, O., Science of Synthesis, (2021) , 47. 摘要:Galczynski, J.; Huang, H.; Lambert, T. H., Science of Synthesis: Special Topics, (2021) 1, 330. 参考文献:10.1093/jac/dkh280 摘要:Espinosa A, Clark D, Stanley SL. Entamoeba histolytica alcohol dehydrogenase 2 (EhADH2) as a target for anti-amoebic agents. J Antimicrob Chemother. 2004 Jul;54(1):56–9. doi: 10.1093/jac/dkh280.