1-烯丙基-4-氟苯置于叔丁基过氧化氢,Palladium Diacetate,对甲苯磺酸体系中,用 水,乙腈 作为反应溶剂,化学反应 6.0H,以95%的收率获得产物4'-氟苯丙酮 参考文献:Direct Conversion Of Allyl Arenes To Aryl Ethylketones Via A Tbhp-Mediated Palladium-Catalyzed Tandem Isomerization-wacker Oxidation Of Terminal Alkenes 标题:Direct Conversion Of Allyl Arenes To Aryl Ethylketones Via A Tbhp-Mediated Palladium-Catalyzed Tandem Isomerization-wacker Oxidation Of Terminal Alkenes 摘要:通过tbhp介导的钯催化串联异构化-Wacker氧化反应,成功开发了对末端烯烃的反应. DOI:10.1039/c5Ob00586H
专利号:US-9409879-B2 优先权日:2011-03-29 标 题 :Total synthesis of redox-active 1.4-naphthoquinones and their metabolites and their therapeutic use as antimalarial and schistomicidal agents 发明人:DAVIOUD-CHARVET ELISABETH; LANFRANCHI DON ANTOINE; JOHANN LAURE; WILLIAMS DAVID LEE; CESAR RODO ELENA 权利人:DAVIOUD-CHARVET ELISABETH; LANFRANCHI DON ANTOINE; JOHANN LAURE; WILLIAMS DAVID LEE; CESAR RODO ELENA; CENTRE NAT RECH SCIENT 摘要:Naphthoquinones, azanaphthoquinones and benxanthones, their process of synthesis and methods of their use as antimalarial or antischistosomal agents.
专利号:US-2008280855-A1 优先权日:2005-06-22 标 题 :Process For the Production of Intermediates For the Preparation of Tricyclic Benzimidazoles 发明人:CHIESA MARIA VITTORIA; PALMER ANDREAS; BUHR WILM; ZIMMERMANN PETER JAN; BREHM CHRISTOF; SIMON WOLFGANG-ALEXANDER; POSTIUS STEFAN; KROMER WOLFGANG; ZANOTTI-GEROSA ANTONIO 权利人:NYCOMED GMBH 摘要:The invention relates to a process for the synthesis of compounds of the formula 1-a and compounds of the formula 1-b. n n n n n n n n n n The compounds of the formula 1-a and the compounds of the formula 1-b, in which the substituents R1, R2, R3, and Ar have the meanings indicated in the description, are valuable intermediates for the preparation of pharmaceutically active compounds.
专利号:WO-9941229-A1 优先权日:1998-02-11 标题:Halogenated phenyl alcohol amides (ligands of gabab receptor) having an anticonvulsant activity 发明人:CARVAJAL SANDOVAL GUILLERMO; MEZA TOLEDO SERGIO ENRIQUE 权利人:CARVAJAL SANDOVAL GUILLERMO; MEZA TOLEDO SERGIO ENRIQUE 摘要:New anticonvulsant compounds have been synthesized with a chlorine or fluorine atom in the position para of the phenyl ring. These compounds include DL-2-hydroxy-2-(4'-chlorophenyl)butyramide, DL-2-hydroxy-2-(4'-fluorophenyl)butyramide, DL-3-hydroxy-3-(4'-chlorophenyl)pentanamide, DL-3-hydroxy-3-(4'-fluorophenyl)pentanamide, DL-4-hydroxy-4-(4'-chlorophenyl)hexanamide and DL-4-hydroxy-4-(4'-fluorophenyl)hexanamide. Said compounds have a rather significant anticonvulsant activity against convulsions produced by pentylene tetrazol, as well as unexpected properties in particular a high affinity to the GABAB receptor in addition to a sustained anticonvulsant activity. The invention also relates to methods for the synthesis of halogenated phenyl alcohol amides such as indicated in the examples given in the disclosure.
专利号:US-8981092-B2 优先权日:2008-09-19 标题 :Substituted 3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-ones as modulators of protein kinase activity 发明人:MIRIZZI DANILO; CERVI GIOVANNI; D ANELLO MATTEO; PAPEO GIANLUCA MARIANO ENRICO; FERGUSON RON; CASUSCELLI FRANCESCO 权利人:MIRIZZI DANILO; CERVI GIOVANNI; D ANELLO MATTEO; PAPEO GIANLUCA MARIANO ENRICO; FERGUSON RON; CASUSCELLI FRANCESCO; NERVIANO MEDICAL SCIENCES SRL 摘要:Compounds which are 4,7-disubstituted derivatives of 3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-one compounds, n nor 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:WO-2012013325-A1 优先权日:2010-07-26 标题 :Process for the preparation of key intermediates for the synthesis of statins or pharmaceutically acceptable salts thereof
专利号:CN-106220495-A 优先权日:2016-08-01 标题 :Method for direct synthesis of unsaturated alkene-containing alpha-acyloxyketone derivatives by α-functionalization reaction of ketones