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Application of Pd-Catalyzed Cross-Coupling Reactions in the Synthesis of 5,5-Dimethy1-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazoles that Inhibit ALK5 Kinase

The result's identifiers

  • Result code in IS VaVaI

    <a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61389030%3A_____%2F16%3A00468499" target="_blank" >RIV/61389030:_____/16:00468499 - isvavai.cz</a>

  • Alternative codes found

    RIV/61989592:15310/16:33162449

  • Result on the web

    <a href="http://dx.doi.org/10.1021/acs.joc.6b02230" target="_blank" >http://dx.doi.org/10.1021/acs.joc.6b02230</a>

  • DOI - Digital Object Identifier

    <a href="http://dx.doi.org/10.1021/acs.joc.6b02230" target="_blank" >10.1021/acs.joc.6b02230</a>

Alternative languages

  • Result language

    angličtina

  • Original language name

    Application of Pd-Catalyzed Cross-Coupling Reactions in the Synthesis of 5,5-Dimethy1-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazoles that Inhibit ALK5 Kinase

  • Original language description

    C-H activation of position 3 of a substituted pyrazole ring catalyzed by palladium(II) was straightforward and convenient for arylated or heteroarylated 5,5-dimethyl-5,6dihydro-4H-pyrrolo[1,2-b]pyrazoles. Moreover, we introduced simple protection of the nitrogen in the pyridin-2-yl directing group, which otherwise does not allow a cross-coupling reaction, by transformation to the N-oxide. Selected final products were reasonably selective ALK5 kinase inhibitors.

  • Czech name

  • Czech description

Classification

  • Type

    J<sub>x</sub> - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)

  • CEP classification

    FR - Pharmacology and apothecary chemistry

  • OECD FORD branch

Result continuities

  • Project

    <a href="/en/project/GA15-15264S" target="_blank" >GA15-15264S: Targeted Transport of Purine Cyclin-dependent Kinase Inhibitors into Cancer Cells</a><br>

  • Continuities

    I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Others

  • Publication year

    2016

  • Confidentiality

    S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Data specific for result type

  • Name of the periodical

    Journal of Organic Chemistry

  • ISSN

    0022-3263

  • e-ISSN

  • Volume of the periodical

    81

  • Issue of the periodical within the volume

    23

  • Country of publishing house

    US - UNITED STATES

  • Number of pages

    16

  • Pages from-to

    11841-11856

  • UT code for WoS article

    000389396400032

  • EID of the result in the Scopus database