2-[(4-硝基苯氧基)甲基]环氧乙烷置于palladium On Activated Charcoal 硫酸,氢气,三乙胺体系中,用 乙醇,二氯甲烷 作为反应溶剂,化学反应 137.0H,反应生成 甲磺司特 参考文献:Synthesis And Antiallergic Activity Of Dimethyl-2-(Phenylcarbamoyl)Ethylsulfonium P-Toluenesulfonate Derivatives 标题:Synthesis And Antiallergic Activity Of Dimethyl-2-(Phenylcarbamoyl)Ethylsulfonium P-Toluenesulfonate Derivatives 摘要:The Derivatives Of Dimethyl-2-(Phenylcarbamoyl)Ethylsulfonium P-Toluenesulfonates Were Synthesized And Evaluated For Antiallergic Activity. The 2,3-Dihydroxyethoxy Group Was Introduced To The Phenyl Ring From The Standpoint Of Lipophilicity And Electronic Effects Of Substituent. The Ige-Induced Rat Passive Cutaneous Anaphylaxis (Pca) Was Inhibited By Oral Administration Of Several Substituted 2-[(4-Propoxyphenyl)Carbamoyl]Ethyldimethylsulfonium P-Toluenesulfonate Derivatives. Among Them (+/-)-2-[4-(3-Ethoxy-2-Hydroxypropoxy)Phenyl]-Carbamoyl]Ethyldimethylsulfonium P-Toluenesulfonate (1A,Ipd-1151T) Was Found To Possess Considerable Activity In The Pca Test,And It Was Launched As Suplatast Tosilate In Japan. DOI:10.1021/jm970285Z
专利号:US-10906888-B2 优先权日:2016-07-14 标 题:Pyrimidine carboxamides as inhibitors of Vanin-1 enzyme 发明人:CASIMIRO-GARCIA AGUSTIN; STROHBACH JOSEPH WALTER; HEPWORTH DAVID; LOVERING FRANK ELDRIDGE; CHOI CHULHO; ALLAIS CHRISTOPHE PHILIPPE; WRIGHT STEPHEN WAYNE 权利人:PFIZER 摘要:Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
专利号:US-10308615-B2 优先权日:2015-05-29 标 题:Heterocyclic compounds as inhibitors of Vanin-1 enzyme 发明人:CASIMIRO-GARCIA AGUSTIN; CONDON JEFFREY SCOTT; FLICK ANDREW CHRISTOPHER; GOPALSAMY ARIAMALA; KIRINCICH STEVEN J; MATHIAS JOHN PAUL; STROBACH JOSEPH WALTER; XIANG JASON SHAOYUN; XING LI HUANG; WANG XIAOLUN 权利人:PFIZER 摘要:Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of n nas defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
专利号:US-2018230127-A1 优先权日:2015-08-13 标题 :Bicyclic-Fused Heteroaryl Or Aryl Compounds 发明人:ANDERSON DAVID RANDOLPH; CURRAN KEVIN JOSEPH; GAVRIN LORI KRIM; GOLDBERG JOEL ADAM; LEE ARTHUR; LOWE MICHAEL DENNIS; PATNY AKSHAY; PIERCE BETSY SUSAN; SAIAH EDDINE; TRZUPEK JOHN DAVID 权利人:PFIZER 摘要:Compounds, tautomers and pharmaceutically acceptable salts of the compounds of Formula (Ia) are disclosed which are inhibitors of Interleukin-1 receptor associated kinase (IRAK4). Methods of treatment, methods of synthesis, and intermediates are also disclosed as defined in the specification.
专利号:US-10316018-B2 优先权日:2015-08-27 标题 :Bicyclic-fused heteroaryl or aryl compounds as IRAK4 modulators 发明人:LEE KATHERINE LIN; ALLAIS CHRISTOPHE PHILIPPE; DEHNHARDT CHRISTOPH MARTIN; GAVRIN LORI KRIM; HAN SEUNGIL; HEPWORTH DAVID; LEE ARTHUR; LOVERING FRANK ELDRIDGE; MATHIAS JOHN PAUL; OWEN DAFYDD RHYS; PAPAIOANNOU NIKOLAOS; SAIAH EDDINE; STROHBACH JOSEPH WALTER; TRZUPEK JOHN DAVID; WRIGHT STEPHEN WAYNE; ZAPF CHRISTOPH WOLFGANG 权利人:PFIZER 摘要:Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia, n nas defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
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合成参考文献
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