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Modification of Boc-Protected CAN508 via Acylation and Suzuki-Miyaura Coupling

M. Pisár, E. Schütznerová, F. Hančík, I. Popa, Z. Trávníček, P. Cankař,

. 2018 ; 23 (1) : . [pub] 20180112

Jazyk angličtina Země Švýcarsko

Typ dokumentu časopisecké články

Perzistentní odkaz   https://www.medvik.cz/link/bmc19028621

The cyclin-dependent kinase inhibitor, CAN508, was protected with di-tert-butyl dicarbonate to access the amino-benzoylated pyrazoles. The bromo derivatives were further arylated by Suzuki-Miyaura coupling using the XPhos Pd G2 pre-catalyst. The coupling reaction provided generally the para-substituted benzoylpyrazoles in the higher yields than the meta-substituted ones. The Boc groups were only utilized as directing functionalities for the benzoylation step and were hydrolyzed under conditions of Suzuki-Miyaura coupling, which allowed for elimination of the additional deprotection step.

Citace poskytuje Crossref.org

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