Nesi Marcella, Borghi Daniela, Brasca Maria Gabriella, Fiorentini Francesco, Pevarello Paolo
Department of Chemistry, Oncology Business Unit, Nerviano Medical Sciences, Viale Pasteur 10-20014 Nerviano, MI, Italy.
Bioorg Med Chem Lett. 2006 Jun 15;16(12):3205-8. doi: 10.1016/j.bmcl.2006.03.051. Epub 2006 Apr 17.
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.
本文介绍了一种强效3-氨基吡唑CDK2/细胞周期蛋白A抑制剂主要代谢物的合成方法。采用了一种从苹果酸开始的立体保守方法来构建羟基取代的吡咯烷酮部分。在合成的关键步骤中，使用固定在Amberlyst 26上的氰基硼氢化钠在三氟乙醇中作为传统溶液相还原剂的有效替代方法。
