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Polymer-Supported Synthesis of Various Pteridinones and Pyrimidodiazepinones.

ABSTRACT: 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.

SUBMITTER: Chasak J

PROVIDER: S-EPMC8000973 | biostudies-literature | 2021 Mar

REPOSITORIES: biostudies-literature

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Polymer-Supported Synthesis of Various Pteridinones and Pyrimidodiazepinones.

Chasák Jan J Brulíková Lucie L

Molecules (Basel, Switzerland) 20210314 6

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 pharmacokinet ...[more]

PMID: 33799340

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