专利号:US-5077408-A 优先权日:1989-09-20 标 题 :Process for the synthesis of oxazolopyridine compounds 发明人:GUILLAUMET GERALD; FLOUZAT CHRISTINE 权利人:SCIENCE ORGANISATION 摘要:Process for the synthesis of compounds of formula (I): ##STR1## their pyridinium salts and N-oxides, in which formula: the nitrogen of the pyridine ring is situated in the α-, β-, γ- or δ-position with respect to the ring junction; n R 1 represents a halogen, a substituted or unsubstituted alkyl, a substituted or unsubstituted alkoxy or a nitro, substituted or unsubstituted amino, phenyl or cyano group; n 0≦m≦2; n R 2 represents a lower alkyl or cycloalkyl group, a 5- or 6-membered heterocycle containing 1 or 2 hetero atoms, substituted or otherwise, or an aryl group ##STR2## such that: R 3 represents a halogen, a substituted or unsubstituted alkyl, a substituted or unsubstituted alkoxy or a nitro, phenyl, substituted or unsubstituted sulfonyl, cyano, thioalkyl, substituted or unsubstituted amino, substituted or unsubstituted sulfinyl, mercapto, hydroxyl or ester group, n 0≦n≦5 n employing trimethylsilyl polyphosphate (PPSE) as a cyclization agent and enabling the compounds of formula (I) to be obtained in virtually quantitative yields. The compounds of formula I have anti-inflammatory, analgesic, and antipyretic activity.
专利号:WO-0005212-A1 优先权日:1998-07-21 标 题:3-substituted pyridine compounds and related synthesis 发明人:HOGLEN DEAN KENT 权利人:NOVARTIS AG; NOVARTIS ERFIND VERWALT GMBH; HOGLEN DEAN KENT 摘要:The present invention relates to 3-substituted and 2,3-disubstituted pyridine compounds of formula (I), wherein R1 is C1-C4 haloalkyl and R4 is H, halogen or C1-C4 alkylthio; and acid addition salts thereof which are useful as intermediates in the synthesis of pyridylsulfonylurea herbicides. The invention also relates to arylation of alcohols using a pyridinediazonium salt. More particularly the arylation process of the instant invention relates to the synthesis of 2,3-disubstituted pyridine compounds via anhydrous diazotization of 3-aminopyridines to form a diazonium salt intermediate that is then reacted with the appropriate alcohol to produce the desired product. The invention additionally relates to pyridine-3-diazonium salt intermediates.
专利号:US-9574189-B2 优先权日:2005-12-01 标题:Enzymatic encoding methods for efficient synthesis of large libraries 发明人:FRANCH THOMAS; LUNDORF MIKKEL DYBRO; JACOBSEN SØREN NYBOE; OLSEN EVA KAMPMANN; ANDERSEN ANNE LEE; HOLTMANN ANETTE; HANSEN ANDERS HOLM; SØRENSEN ANDERS MALLING; GOLDBECH ANNE; DE LEON DAEN; KALDOR DITTE KIEVSMOSE; SLØK FRANK ABILDGAARD; HUSEMOEN GITTE NYSTRUP; DOLBERG JOHANNES; Jensen Kim Birkebæ; PEDERSEN LENE; NØRREGAARD-MADSEN MADS; GODSKESEN MICHAEL ANDERS; GLAD SANNE SCHRØDER; NEVE SØREN; THISTED THOMAS; KRONBORG TINE TITILOLA AKINLEMINU; SAMS CHRISTIAN KLARNER; FELDING JAKOB; FRESKGÃ…RD PER-OLA; GOULIAEV ALEX HAAHR; PEDERSEN HENRIK 权利人:FRANCH THOMAS; LUNDORF MIKKEL DYBRO; JACOBSEN SØREN NYBOE; OLSEN EVA KAMPMANN; ANDERSEN ANNE LEE; HOLTMANN ANETTE; HANSEN ANDERS HOLM; SØRENSEN ANDERS MALLING; GOLDBECH ANNE; DE LEON DAEN; KALDOR DITTE KIEVSMOSE; SLØK FRANK ABILDGAARD; HUSEMOEN GITTE NYSTRUP; DOLBERG JOHANNES; Jensen Kim Birkebæ; PEDERSEN LENE; NØRREGAARD-MADSEN MADS; GODSKESEN MICHAEL ANDERS; GLAD SANNE SCHRØDER; NEVE SØREN; THISTED THOMAS; KRONBORG TINE TITILOLA AKINLEMINU; SAMS CHRISTIAN KLARNER; FELDING JAKOB; FRESKGÃ…RD PER-OLA; GOULIAEV ALEX HAAHR; PEDERSEN HENRIK; NUEVOLUTION AS 摘要:Disclosed is a method for obtaining a bifunctional complex comprising a molecule linked to a single stranded identifier oligonucleotide, wherein a nascent bifunctional complex comprising a chemical reaction site and a priming site for enzymatic addition of a tag is a) reacted at the chemical reaction site with one or more reactants, and b) reacted enzymatically at the priming site with one or more tag(s) identifying the reactant(s).
专利号:US-4897484-A 优先权日:1986-12-19 标题 :Process for the preparation of substituted pyridines 发明人:WEIS CLAUS D; SUTTER PETER 权利人:CIBA GEIGY CORP 摘要:A process is described for the preparation of compounds of the formula (1) in which R and X are as defined in claim 1. The compounds of the formula (1) are valuable intermediates in the synthesis of triarylmethane dyes and triarylmethanelactones.
专利号:US-5010198-A 优先权日:1984-12-03 标题:Intermediates for the synthesis of benzoxazol- and benzothiazolamine derivatives, useful as anti-anoxic agents 发明人:STOKBROEKX RAYMOND A; LUYCKX MARCEL G M; JANSSENS FRANS E 权利人:JANSSEN PHARMACEUTICA NV 摘要:Benzoxazol- and benzothiazolamine derivatives having anti-anoxic properties which compounds are useful in the treatment of anoxia. These compounds are produced from certain benzoxazol- and benzothizolamine intermediates.
专利号:US-6943254-B2 优先权日:1997-03-07 标 题 :Synthesis of pyrazinyl pyridine-3-sulfonamide compounds 发明人:HOGAN PHILIP JOHN 权利人:ASTRAZENECA UK LTD 摘要:A process for the manufacture of: n n nwherein R is (1-4C)alkyl, carboxyl(1-4C)alkyl or 1,3,4-oxadiazol-2-yl comprises:n (a) reaction of the diazonium salt of 3-amino-2-chloropyridine with thionyl chloride in water and an electron transfer catalyst; (b) reaction with isobutyl-(3-methoxy-5-methylpyrazin-2-yl)carbamate and an alkali metal hydride in inert solvent; and (I) where R is (1-4C)alkyl, carboxy(1-4C)alkyl: (c) reaction with a boronic acid: n n (or an anhydride or ester therof) in the presence of a base and a palladium or nickel catalyst in solvent; and removal of the isobutoxy carbonyl group; or (ii) where R is 1,3,4-oxadiazol-2-yl (c) reaction with 4-methoxycarbonylphenylboronic acid (or an anhydride or ester thereof) with a source fluoride ion under aqueous conditions; (d) removal of the isobutoxycarbonyl protecting group; (e) conversion of the methyl ester group to the hydrazide; and (f) conversion to a 1,3,4-oxadiazol-2-yl moiety.
参考标题:Palladium-Catalyzed Carbonylation Of 2-Bromoanilines With 2-Formylbenzoic Acid And 2-Halobenzaldehydes: Efficient Synthesis Of Functionalized Isoindolinones 作者:Kishore Natte,Jianbin Chen,Haoquan Li,Helfried Neumann,Matthias Beller,Xiao-Feng Wu |发布日期:2014.10.27 摘要:Versatile Method For The Synthesis Of Functionalized Isoindolinones Is Reported. Various 2‐bromoanilines Undergo Palladium‐catalyzed Carbonylation With 2‐formylbenzoic Acid Under A Convenient And Mild Procedure To Give Good To Excellent Yields Of The Corresponding Isoindolinones. Additionally, 2‐halobenzaldehydes Can Be Applied As Substrates In Palladium‐catalyzed Double‐carbonylation To Provide Identical