专利号:US-9096519-B2 优先权日:2013-01-10 标 题 :Process for the synthesis of ketones from internal alkenes 发明人:MORANDI BILL; GRUBBS ROBERT H; WICKENS ZACHARY K; LERCH MICHAEL M 权利人:CALIFORNIA INST OF TECHN 摘要:The present invention is directed to methods for oxidizing internal olefins to ketones. In various embodiments, each method comprising contacting an organic substrate, having an initial internal olefin, with a mixture of (a) a biscationic palladium salt; and (b) an oxidizing agent; dissolved or dispersed in a solvent system to form a reaction mixture, said solvent system comprising at least one C 2-6 carbon nitrile and optionally at least one secondary alkyl amide, said method conducted under conditions sufficient to convert at least 50 mol % of the initial internal olefin to a ketone, said ketone positioned on a carbon of the initial internal olefin. The transformation occurs at room temperature and shows wide substrate scope. Applications to the oxidation of seed oil derivatives and a bioactive natural product are described.
专利号:US-9988368-B1 优先权日:2017-06-16 标题:Chiral synthesis method for producing cis-imidazoline compounds for pharmaceutical use 发明人:VON GELDERN THOMAS W; BACKES BRADLEY; CHEN BING 权利人:UNITY BIOTECHNOLOGY INC 摘要:This invention provides a method for enantioselective synthesis of cis-imidazolines and related structures through chiral resolution. A chiral acid is used to separate enantiomeric precursors of the cis-imidazolines from a racemic mixture by selective crystallization. Both enantiomers can be cyclized into the desired cis-imidazoline by complementary pathways. Compounds can be synthesized according to the invention with an enantiomeric excess as high as 99%. Cis-imidazolines such as Nutlin-3a prepared according to this invention may be used for treating cancer, killing senescent cells, or treating senescence-associated conditions.
专利号:US-6225463-B1 优先权日:1997-12-22 标 题 :Synthesis of new β-lactams 发明人:DE VOS DICK; BROWN STEPHEN; JORDAN ALLAN M; LAWRENCE NICHOLAS J; MCGOWN ALAN TH 权利人:PHARMACHEMIE BV; CANCER RES CAMPAIGN TECH 摘要:The object of the present invention is the development of new chiral auxiliaries for improved beta-lactam formation that control both the diastereoselectivity of beta-lactam formation and which can be removed without destruction of the sensitive azetidinone ring, providing valuable intermediates for coupling to the C-13 hydroxyl group of anti-tumor taxanes, such as paclitaxel. Further, the object of the present invention is enantiomerically pure (S)-(-)-1-(p-methoxy-phenyl)propyl-1-amine.
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: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
参考标题:A Metal-Free Approach For The Synthesis Of 2-Tetralones Via Carbanion-Induced Ring Transformation Of 2H-Pyran-2-Ones 作者:Fateh Singh,Samata Shetgaonkar |发布日期:2018.9 摘要:Economical And Tolerates A Wide Range Of Functional Groups. A Metal-Free, Ultrasound-Assisted Approach For The Synthesis Of Highly Functionalized 2-Tetralones In High Yields Is Described. The Process Involves Ring Transformation Of 2H-Pyran-2-Ones With The Spirocyclic Ketone 1,4-Cyclohexandione Monoethylene Ketal To Yield SpiroCyclic Ketals And Subsequent Acid-Mediated Hydrolysis. This Protocol Is Free From
合成参考文献
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