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10070-92-5 4595-61-3 34253-01-5欧盟法规
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CAS号10070-92-5 5-嘧啶甲醛 | CAS号40929-50-8 嘧啶-5-甲酸乙酯 | CAS号496-13-9 2,3-二氢-1H-吡咯[3,... | CAS号147740-04-3 2,3-二氢-1H-吡咯[3,... | CAS号101346-02-5 5-氯甲基嘧啶5-嘧啶甲酸乙酯置于lithium Aluminium Tetrahydride体系中,用 四氢呋喃 用作溶剂,化学反应生成5-嘧啶甲醇
参考文献:Discovery Of Ritonavir,A Potent Inhibitor Of Hiv Protease With High Oral Bioavailability And Clinical Efficacy
标题:Discovery Of Ritonavir,A Potent Inhibitor Of Hiv Protease With High Oral Bioavailability And Clinical Efficacy
摘要:The Structure-Activity Studies Leading To The Potent And Clinically Efficacious Hiv Protease Inhibitor Ritonavir Are Described. Beginning With The Moderately Potent And Orally Bioavailable Inhibitor A-80987,Systematic Investigation Of Peripheral (P3 And P2') Heterocyclic Groups Designed To Decrease The Rate Of Hepatic Metabolism Provided Analogues With Improved Pharmacokinetic Properties After Oral Dosing In Rats. Replacement Of Pyridyl Groups With Thiazoles Provided Increased Chemical Stability Toward Oxidation While Maintaining Sufficient Aqueous Solubility For Oral Absorption,Optimization Of Hydrophobic Interactions With The Hiv Protease Active Site Produced Ritonavir,With Excellent In Vitro Potency (Ec50 = 0.02 Mu M) And High And Sustained Plasma Concentrations After Oral Administration In Four Species. Details Of The Discovery And Preclinical Development Of Ritonavir Are Described.
Doi:10.1021/jm970636+
专利信息
专利号:US-3869456-A
优先权日:1972-03-13
标 题 :Synthesis of 5-pyrimidinecarbinols
发明人:TAYLOR HAROLD M; DAVENPORT JAMES D; HACKLER RONALD E
权利人:LILLY CO ELI
摘要:There is disclosed an improved method of synthesizing 5pyrimidinecarbinols by the addition of an alkyllithium to a mixture of 5-halopyrimidine and a ketone at a low temperature. The product compounds are useful as plant fungicides and as plant growth regulators.
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:CN-115819408-A
优先权日:2022-10-21
标 题 :A method for highly selective synthesis of key intermediates of rosuvastatin
专利号:US-2008176865-A1
优先权日:2005-06-15
标 题:Substituted arylpyrazoles
发明人:BILLEN DENIS; BOYLE JESSICA; CRITCHER DOUGLAS JAMES; GETHIN DAVID MORRIS; HALL KIM THOMAS; KYNE GRAHAM MICHAEL
权利人:PFIZER LTD
摘要:This invention relates to a range of 1-aryl-4-cyclopropylpyrazoles in which the cyclopropyl ring is substituted at the angular position, and pharmaceutically acceptable salts and solvates thereof, to compositions comprising such compounds, processes to their synthesis and their use as parasiticides.
专利号:US-7645786-B2
优先权日:2005-06-15
标题:Substituted arylpyrazoles
发明人:BILLEN DENIS; BOYLE JESSICA; CRITCHER DOUGLAS JAMES; GETHIN DAVID MORRIS; HALL KIM THOMAS; KYNE GRAHAM MICHAEL
权利人:PFIZER
摘要:This invention relates to a range of 1-aryl-4-cyclopropylpyrazoles in which the cyclopropyl ring is substituted at the angular position, and pharmaceutically acceptable salts and solvates thereof, to compositions comprising such compounds, processes to their synthesis and their use as parasiticides.