专利号:US-8138272-B2 优先权日:2006-05-22 标 题:Preparation of polymer conjugates of therapeutic, agricultural, and food additive compounds 发明人:KONRADI ANDREI W; SMITH JENIFER L 权利人:KONRADI ANDREI W; SMITH JENIFER L; ELAN PHARM INC 摘要:This invention provides an improved synthesis of polymer conjugates of formula (I), n nof agricultural, therapeutic, and food additive compounds. In particular, a process is described for the preparation of conjugates by treating primary or secondary alcohol substituents of active compounds with polymeric nucleophiles using “Mitsunobuâ€? or related reaction conditions.
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.
专利号:US-8697888-B2 优先权日:2012-01-06 标题 :Substituted (1-(methylsulfonyl)azetidin-3-yl)(heterocycloalkyl)methanone analogs as antagonists of muscarinic acetylcholine M1 receptors 发明人:LINDSLEY CRAIG W; CONN P JEFFREY; WOOD MICHAEL R; MELANCON BRUCE J; CHEUNG YIU-YIN 权利人:UNIV VANDERBILT 摘要:In one aspect, the invention relates to substituted (1-(methylsulfonyl)azetidin-3-yl)(heterocycloalkyl)methanone analogs, derivatives thereof, and related compounds, which are useful as antagonists of the muscarinic acetylcholine receptor M 1 (mAChR M 1 ); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
专利号:US-5521179-A 优先权日:1991-04-18 标题 :Heterocyclic amides 发明人:BERNSTEIN PETER R; SHAW ANDREW; THOMAS ROYSTON M; WARNER PETER; WOLANIN DONALD J 权利人:ZENECA LTD 摘要:The present invention relates to certain novel heterocyclic amides which are 1-pyridylacetamide compounds of formula I, set out herein, which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes intermediates useful in the synthesis of these heterocyclic amides, processes for preparing the heterocyclic amides, pharmaceutical compositions containing such heterocyclic amides and methods for their use.
专利号:EP-0630382-B1 优先权日:1992-04-16 标题 :Lactam dipeptides having hle inhibiting activity 发明人:BERSTEIN PETER ROBERT; THOMAS ROYSTON MARTIN; WARNER PETER; WOLANIN DONALD JOHN 权利人:ZENECA LTD 摘要:The present invention relates to certain novel heterocyclic compounds which are 1-pyridylacetamide compounds of formula (I), set out herein, which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes intermediates useful in the synthesis of these heterocyclic compounds, processes for preparing the heterocyclic compounds, pharmaceutical compositions containing such heterocyclic compounds and methods for their use.
专利号:UA-68408-C2 优先权日:1998-12-23 标 题:3-azabicyclo[3.1.0]hexane derivatives as opiate receptor ligands, pharmaceutical and veterinary composition, method for treatment and method for synthesis of derivatives
参考标题:Cobalt(II)-Catalyzed Isocyanide Insertion Reaction With Sulfonyl Azides In Alcohols: Synthesis Of Sulfonyl Isoureas 作者:Tian Jiang,Zheng-Yang Gu,Ling Yin,Shun-Yi Wang,Shun-Jun Ji |发布日期:2017.8.4 摘要:A Co(II)-Catalyzed Isocyanide Insertion Reaction With Sulfonyl Azides In Alcohols To Form Sulfonyl Isoureas Via Nitrene Intermediate Has Been Developed. This Protocol Provides A New, Environmentally Friendly, And Simple Strategy For The Synthesis Of Sulfonyl Isourea Derivatives By Employing A Range Of Substrates Under Mild Conditions.
合成参考文献
摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2025). 摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2025). 摘要:Cellnik, T.; Jo, W.; Healy, A., Science of Synthesis: Knowledge Updates, (2024) 2, 353. 摘要:Kwiatkowska, M.; Kiełbasiński, P., Science of Synthesis: Knowledge Updates, (2024) 3, 419.