Synthesis of dihydrouracils spiro-fused to pyrrolidines: druglike molecules based on the 2-arylethyl amine scaffold

与吡咯烷螺合的二氢尿嘧啶的合成:基于 2-芳基乙胺骨架的类药物分子

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作者:Daniel Blanco-Ania, Carolina Valderas-Cortina, Pedro H H Hermkens, Leo A J M Sliedregt, Hans W Scheeren, Floris P J T Rutjes

Abstract

The synthesis of a small library of dihydrouracils spiro-fused to pyrrolidines is described. These compounds are synthesized from beta-aryl pyrrolidines, providing products with the 2-arylethyl amine moiety, a structural feature often encountered in compounds active in the central nervous system. The b-aryl pyrrolidines are synthesized through a three-step methodology that includes a Knoevenagel condensation reaction, a 1,3-dipolar cycloaddition reaction, and a nitrile reduction.

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