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A practical synthesis of the major 3-hydroxy-2-pyrrolidinone metabolite of a potent CDK2/cyclin A inhibitor. | LitMetric

A practical synthesis of the major 3-hydroxy-2-pyrrolidinone metabolite of a potent CDK2/cyclin A inhibitor.

Bioorg Med Chem Lett

Department of Chemistry, Oncology Business Unit, Nerviano Medical Sciences, Viale Pasteur 10-20014 Nerviano, MI, Italy.

Published: June 2006

The synthesis of the major metabolite of a potent 3-aminopyrazole CDK2/cyclin A inhibitor is presented. A stereoconservative approach starting from malic acid was employed to construct the hydroxy-substituted pyrrolidinone moiety. In the key step of the synthesis the use of cyanoborohydride immobilized on Amberlyst 26 in trifluoroethanol represented a valid alternative to conventional solution-phase reducing agents.

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http://dx.doi.org/10.1016/j.bmcl.2006.03.051DOI Listing

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