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One-pot synthesis of 2-aryl-1,2-fused pyrimidones

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Abstract

A facile and versatile method for the synthesis of alicyclic fused pyrimidones from aminoacrylates and lactams in the presence of phosphorous oxychloride is described. The results suggest that this method is widely applicable except for cyclobutyl fused systems. This method gives better yield than the method of condensing aminopyrrolidines with the beta keto esters.

Synthesis and characterization of twenty five 2-aryl-1,2-fused pyrimidone derivatives are reported. The results suggested that the methodology is widely applicable except for cyclobutyl fused systems. This method gives better yield and more versatile than the method of condensing aminopyrrolidines with the beta keto esters.

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Acknowledgements

Authors thank Department of Discovery Analytical Services of Biocon Bristol-Myers Squibb Research Center for their valuable support and, Jianqing Li, Richard Rampulla and Bei Wang of Bristol Myers Squibb for logistic help.

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Correspondence to PIRAMA NAYAGAM ARUNACHALAM.

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Supplementary Information (SI)

Characerization data and Figures S1S25 for all the compounds are provided in the Supplementary Information which is available at www.ias.ac.in/chemsci.

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RAMESH, S., SARAVANAKUMAR, P., DURAISAMY, R. et al. One-pot synthesis of 2-aryl-1,2-fused pyrimidones. J Chem Sci 129, 329–333 (2017). https://doi.org/10.1007/s12039-017-1244-z

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