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Keywords = spiro dihydrouracils

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33 pages, 300 KB  
Article
Synthesis of Dihydrouracils Spiro-Fused to Pyrrolidines: Druglike Molecules Based on the 2-Arylethyl Amine Scaffold
by Daniel Blanco-Ania, Carolina Valderas-Cortina, Pedro H.H. Hermkens, Leo A.J.M. Sliedregt, Hans W. Scheeren and Floris P.J.T. Rutjes
Molecules 2010, 15(4), 2269-2301; https://doi.org/10.3390/molecules15042269 - 30 Mar 2010
Cited by 16 | Viewed by 14652
Abstract
The synthesis of a small library of dihydrouracils spiro-fused to pyrrolidines is described. These compounds are synthesized from b-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 [...] Read more.
The synthesis of a small library of dihydrouracils spiro-fused to pyrrolidines is described. These compounds are synthesized from b-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. Full article
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