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Polymer-Supported Synthesis of Various Pteridinones and Pyrimidodiazepinones

J. Chasák, L. Brulíková

. 2021 ; 26 (6) : . [pub] 20210314

Jazyk angličtina Země Švýcarsko

Typ dokumentu časopisecké články

Perzistentní odkaz   https://www.medvik.cz/link/bmc21019049

Grantová podpora
IGA_PrF_2020_012 Univerzita Palackého v Olomouci
IGA_PrF_2021_024 Univerzita Palackého v Olomouci

In this report, we employed the solid-phase synthetic approach to prepare variously substituted dihydropteridinones, tetrahydropyrrolopteridinones, and pyrimidodiazepinones, using a versatile building block-4,6-dichloro-5-nitropyrimidine. All these compounds are pharmacologically significant scaffolds of the great importance of medicinal chemists. The fast and efficient synthetic methodology is highly desirable for defining their structure-activity relationship (SAR) and optimizing pharmacokinetic properties. Our research efforts utilize simple synthetic methods to generate a library of analogues for future SAR studies. The efficiency of our approach was exemplified in various pteridinones as well as pyrimidodiazepinones.

Citace poskytuje Crossref.org

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