Tert-Butyl 2-(2,2,2-Trifluoroethyl)Hydrazinecarboxylate置于三氟乙酸体系中,用 二氯甲烷 作为反应溶剂,化学反应生成 2,2,2-三氟乙基肼 参考文献:Discovery,Synthesis And Characterization Of A Series Of (1-Alkyl-3-Methyl-1H-Pyrazol-5-yl)-2-(5-Aryl-2H-Tetrazol-2-yl)Acetamides As Novel Girk1/2 Potassium Channel Activators 标题:Discovery,Synthesis And Characterization Of A Series Of (1-Alkyl-3-Methyl-1H-Pyrazol-5-yl)-2-(5-Aryl-2H-Tetrazol-2-yl)Acetamides As Novel Girk1/2 Potassium Channel Activators 摘要:The Present Study Describes The Discovery And Characterization Of A Series Of 5-Aryl-2H-Tetrazol-3-Ylacetamides As G Protein-Gated Inwardly-Rectifying Potassium (Girk) Channels Activators. Working From An Initial Hit Discovered During A High-Throughput Screening Campaign,We Identified A Tetrazole Scaffold That Shifts Away From The Previously Reported Urea-Based Scaffolds While Remaining Effective Girk1/2 Channel Activators. In Addition,We Evaluated The Compounds In Tier 1 Dmpk Assays And Have Identified A (3-Methyl-1H-Pyrazol-1-yl)Tetrahydrothiophene-1,1-Dioxide Head Group That Imparts Interesting And Unexpected Microsomal Stability Compared To Previously-Reported Pyrazole Head Groups. DOI:10.1016/j.Bmcl.2019.01.027
专利号:US-6867202-B1 优先权日:1997-06-25 标 题 :Treatment of insulin resistance 发明人:CARPINO PHILIP ALBERT; CHIU CHARLES KWOK-FUNG; PAN LYDIA CODETTA; LEFKER BRUCE ALLEN; TREADWAY JUDITH LEE; ZAWISTOSKI MICHAEL PAUL 权利人:PFIZER 摘要:This invention is directed to methods of treating insulin resistance in a mammal which comprise administering an effective amount of a compound of formula I, n n nwhere the variables are defined in the specification, or the stereoisomeric mixtures, diastereomerically enriched, diastereomerically pure, enantiomerically enriched or enantiomerically pure isomers, or the pharmaceutically acceptable salts and prodrugs thereof to said mammal. The compounds of formula I are growth hormone secretagogues and as such are useful for increasing the level of endogenous growth hormone. In another aspect this invention provides certain intermediates which are useful in the synthesis of the foregoing compounds and certain processes useful for the synthesis of said intermediates and th compounds of formula I. This invention is further directed to methods comprising administering to a human or other animal a combination of a functional somatostatin antagonist such as an alpha-2 adrenergic agonist and a compound of formula I.
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:US-9192612-B2 优先权日:2013-02-13 标题:Heteroaryl-substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds 发明人:BRODNEY MICHAEL AARON; BUTLER CHRISTOPHER RYAN; BECK ELIZABETH MARY; DAVOREN JENNIFER ELIZABETH; LACHAPELLE ERIK ALPHIE; O'NEILL BRIAN THOMAS 权利人:PFIZER 摘要:The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula I, n nand the variables R 1 and R 2 are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
[参考文献]: Hyun-Ji Kim, Et Al. Simple And Automatic Determination Of Aldehydes And Acetone In Water By Headspace Solid-Phase Microextraction And Gas Chromatography-Mass Spectrometry. J Sep Sci. 2011 Mar;34(6):693-9.
合成参考文献
摘要:R. Pollet and H. V. Eynde. Bull. Soc. Chim. Belg. 77, 371 (1968).