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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
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SYSNO ASEP 0468499 Document Type J - Journal Article R&D Document Type Journal Article Subsidiary J Článek ve WOS Title 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 Author(s) Tenora, L. (CZ)
Galeta, J. (US)
Řezníčková, Eva (UEB-Q) RID, ORCID
Kryštof, Vladimír (UEB-Q) RID, ORCID
Potáček, M. (CZ)Number of authors 5 Source Title Journal of Organic Chemistry. - : American Chemical Society - ISSN 0022-3263
Roč. 81, č. 23 (2016), s. 11841-11856Number of pages 16 s. Language eng - English Country US - United States Keywords c-h functionalization ; pyridine n-oxides ; receptor-type-i ; direct arylation ; tgf-beta ; galunisertib ly2157299 ; domain inhibitors ; bond activation ; growth ; withasomnine Subject RIV FR - Pharmacology ; Medidal Chemistry R&D Projects GA15-15264S GA ČR - Czech Science Foundation (CSF) Institutional support UEB-Q - RVO:61389030 UT WOS 000389396400032 DOI 10.1021/acs.joc.6b02230 Annotation 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. Workplace Institute of Experimental Botany Contact David Klier, knihovna@ueb.cas.cz, Tel.: 220 390 469 Year of Publishing 2017
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