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

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61989592%3A15110%2F18%3A73591041" target="_blank" >RIV/61989592:15110/18:73591041 - isvavai.cz</a>
Alternative codes found
RIV/61989592:15310/18:73591041
Result on the web
<a href="https://www.mdpi.com/1420-3049/23/1/149/htm" target="_blank" >https://www.mdpi.com/1420-3049/23/1/149/htm</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.3390/molecules23010149" target="_blank" >10.3390/molecules23010149</a>

Result language
angličtina
Original language name
Modification of Boc-Protected CAN508 via Acylation and Suzuki-Miyaura Coupling
Original language description
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.
Czech name
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Czech description
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Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
—
OECD FORD branch
10401 - Organic chemistry

Project
Result was created during the realization of more than one project. More information in the Projects tab.
Continuities
P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)<br>S - Specificky vyzkum na vysokych skolach

Publication year
2018
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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