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CuI-catalyzed synthesis of multisubstituted pyrido[1,2-a]pyrimidin-4-ones through tandem Ullmann-type C-N cross-coupling and intramolecular amidation reaction.

ABSTRACT: Various multi-substituted pyrido[1,2-a]pyrimidin-4-ones were synthesized via a one-pot tandem CuI-catalyzed C-N bond formation/intramolecular amidation reaction at 130 °C in DMF. This protocol features simple operation, broad substrate scope, good functional group tolerance and gram scale preparation, thus allowing practical and modular synthesis of pyrido[1,2-a]pyrimidin-4-ones from readily available 2-halopyridine and (Z)-3-amino-3-arylacrylate ester in good to excellent yields.

SUBMITTER: Mo B

PROVIDER: S-EPMC10424054 | biostudies-literature | 2023 Aug

REPOSITORIES: biostudies-literature

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CuI-catalyzed synthesis of multisubstituted pyrido[1,2-a]pyrimidin-4-ones through tandem Ullmann-type C-N cross-coupling and intramolecular amidation reaction.

Mo Baichuan B Chen Chunxia C Peng Jinsong J

RSC advances 20230814 35

Various multi-substituted pyrido[1,2-a]pyrimidin-4-ones were synthesized via a one-pot tandem CuI-catalyzed C-N bond formation/intramolecular amidation reaction at 130 °C in DMF. This protocol features simple operation, broad substrate scope, good functional group tolerance and gram scale preparation, thus allowing practical and modular synthesis of pyrido[1,2-a]pyrimidin-4-ones from readily available 2-halopyridine and (Z)-3-amino-3-arylacrylate ester in good to exce ...[more]

PMID: 37583662

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