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Molecules 2010, 15(4), 2269-2301; doi:10.3390/molecules15042269
Article

Synthesis of Dihydrouracils Spiro-Fused to Pyrrolidines: Druglike Molecules Based on the 2-Arylethyl Amine Scaffold

1, 1, 2, 3, 1 and 1,*
Received: 5 February 2010; in revised form: 26 March 2010 / Accepted: 30 March 2010 / Published: 30 March 2010
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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 are synthesized through a three-step methodology that includes a Knoevenagel condensation reaction, a 1,3-dipolar cycloaddition reaction, and a nitrile reduction.
Keywords: Knoevenagel condensation; 1,3-dipolar cycloaddition; azomethine ylide; parallel synthesis; spiro dihydrouracils Knoevenagel condensation; 1,3-dipolar cycloaddition; azomethine ylide; parallel synthesis; spiro dihydrouracils
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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MDPI and ACS Style

Blanco-Ania, D.; Valderas-Cortina, C.; Hermkens, P.H.; Sliedregt, L.A.; Scheeren, H.W.; Rutjes, F.P. Synthesis of Dihydrouracils Spiro-Fused to Pyrrolidines: Druglike Molecules Based on the 2-Arylethyl Amine Scaffold. Molecules 2010, 15, 2269-2301.

AMA Style

Blanco-Ania D, Valderas-Cortina C, Hermkens PH, Sliedregt LA, Scheeren HW, Rutjes FP. Synthesis of Dihydrouracils Spiro-Fused to Pyrrolidines: Druglike Molecules Based on the 2-Arylethyl Amine Scaffold. Molecules. 2010; 15(4):2269-2301.

Chicago/Turabian Style

Blanco-Ania, Daniel; Valderas-Cortina, Carolina; Hermkens, Pedro H.H.; Sliedregt, Leo A.J.M.; Scheeren, Hans W.; Rutjes, Floris P.J.T. 2010. "Synthesis of Dihydrouracils Spiro-Fused to Pyrrolidines: Druglike Molecules Based on the 2-Arylethyl Amine Scaffold." Molecules 15, no. 4: 2269-2301.


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