5401-15-0Relevant academic research and scientific papers
Preparation method of heterocyclicpyrimidinedione compound
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Paragraph 0066; 0067; 0068, (2018/03/26)
The invention discloses a preparation method of a heterocyclicpyrimidinedione compound and relates to the technology of medicinal chemistry. The preparation method comprises the following steps: 1) mixing an o-amino formonitrile heterocyclic compound and a catalyst to form a mixture, wherein the catalyst is [HDBN][TFE]; 2) in a CO2 environment, heating the mixture and reacting; 3) when the temperature is reduced to room temperature, adjusting the pH value to neutrality, and extracting, separating and collecting the an organic phase; drying, filtering and then vaporizing; performing column chromatography separation to obtain the heterocyclicpyrimidinedione compound. The preparation method disclosed by the invention has the advantages of low cost, environmental friendliness, simple preparation process and wide application range of substrate.
Ionic liquid promoted synthesis of heterocycle-fused pyrimidine-2,4(1H,3H)-diones utilising CO2
Li, Chun,Lu, Xunhua,Yang, Yuanyong,Yang, Shenggang,Zhang, Lin
supporting information, p. 2463 - 2466 (2018/05/26)
An efficient ionic liquid system was developed for the preparation of various heterocycle-fused pyrimidine-2, 4(1H,3H)-diones in moderate to excellent yields (52–95%). It was found that [HDBN+][TFE?], a simple and easily prepared ionic liquid, could act as both the solvent and reaction promoter, and that the reactions could be efficiently carried out at atmospheric pressures of CO2.
Structure-based optimization of pyrazolo-pyrimidine and -pyridine inhibitors of PI3-kinase
Staben, Steven T.,Heffron, Timothy P.,Sutherlin, Daniel P.,Bhat, Seema R.,Castanedo, Georgette M.,Chuckowree, Irina S.,Dotson, Jenna,Folkes, Adrian J.,Friedman, Lori S.,Lee, Leslie,Lesnick, John,Lewis, Cristina,Murray, Jeremy M.,Nonomiya, Jim,Olivero, Alan G.,Plise, Emile,Pang, Jodie,Prior, Wei Wei,Salphati, Laurent,Rouge, Lionel,Sampath, Deepak,Tsui, Vickie,Wan, Nan Chi,Wang, Shumei,Weismann, Christian,Wu, Ping,Zhu, Bing-Yan
scheme or table, p. 6048 - 6051 (2010/11/17)
Starting from HTS hit 1a, X-ray co-crystallization and molecular modeling were used to design potent and selective inhibitors of PI3-kinase. Bioavailablity in this series was improved through careful modulation of physicochemical properties. Compound 12 d
ANTIVIRAL PYRIMIDINES
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Page/Page column 94, (2010/11/03)
Disclosed herein are novel compounds comprising substituted pyrimidines, pyrazolopyrimtdines, and imidazolopyrimidines, the syntheses thereof, and compositions thereof, including pharmaceutical compositions, comprising the novel pyrimidines, pyrazolopyrimtdines, imidazolpyrimidines and related compounds. Such compounds function to inhibit entry of viruses of the Flaviviridae family, including Hepatitis C virus (HCV), into cells that are susceptible to virus infection. These compounds are useful for the treatment, therapy and/or prophylaxis of viral diseases and infection, including HCV infection.
PYRAZOLOPYRIMIDINE PI3K INHIBITOR COMPOUNDS AND METHODS OF USE
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Page/Page column 64, (2009/09/05)
Compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. [Fomula I]
Pyrazolo[3,4-d]pyrimidine compounds and their use as modulators of protein kinase
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Page/Page column 19, (2009/03/07)
The invention relates to pyrazolo[3,4-d]pyrimidine compounds of formual I and its salts wherein the substitents are as defined in the specification, their use for the treatment of protein kinase modulation responsive diseases or in the manufacture of phar
Pyrazolothiazolopyrimidine derivatives as a novel class of anti-inflammatory or antinociceptive agents: synthesis, structural characterization and pharmacological evaluation
Russo, F,Guccione, S,Romeo, G,Barretta, G Uccello,Pucci, S,et al.
, p. 363 - 376 (2007/10/02)
As a part of a research program on anti-inflammatory-analgesic compounds, pyrazolothiazolopyrimidines 5a-f and 5g-i were prepared by cyclodehydration in 98percent H2SO4 or PPA of the corresponding 6-thioketomethylene-substituted-4-hydroxypyrazolopyrimidinies 2a-i and 2g-i.The results of the pharmacological in vivo screening indicate an interesting dissociation of the analgesic from the anti-inflammatory activity depending on aromatic or aliphatic substitution at C4 of the thiazole ring.Analgesic activity was not associated with any narcotic affect: in addition, all th e active compounds showed a remarkable systemic and gastric tolerance.This indicated a mode of action different from that of the classical nonsteroidal anti-inflammatory drugs, acting on prostaglandin biosynthesis.To clarify the mechanism or the mechanisms underlying the pharmacological activity of these and other closely related compounds, we initiated a 'file chemical approach' to various systems involved in the inflammatory process.At present, some of the more active in vivo compounds tested as substance P antagonists showed a moderate and possibly non-specific effect on NK1 and NK2 receptors. pyrazolothiazolopyrimidine derivatives / anti-inflammatory-analgesic activity / substance P antagonists
Heterocyclic β-Enamino Esters, 39. - Synthesis of 1H-Pyrazolopyrimidines
Wamhoff, Heinrich,Ertas, Muemtaz,Atta, Sanaa M. S.
, p. 1910 - 1916 (2007/10/02)
Die Pyrazol-Enaminoester 1a, b und 4-Pyrazolcarbohydrazide 4a, b sind nuetzliche Ausgangsverbindungen fuer die Darstellung von 1H-Pyrazolopyrimidinen.So ergeben Orthoameisensaeure- und Orthoessigsaeure-triethylester mit 4a, b die 5-(Ethoxymethylena
