4-Aminopyrimidine libraries from the Ugi-Smiles reaction of thiouracil |
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| Authors: | Madjid Ait Sidhoum Laurent El Kaïm Laurence Grimaud |
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| Institution: | 1. Laboratoire de Synthèse Organique, CNRS, Ecole Polytechnique, ENSTA ParisTech-UMR 7652, Université Paris-Saclay, 828 Bd des Maréchaux, 91128 Palaiseau, France;2. PASTEUR, Département de Chimie, École Normale Supérieure, PSL University, Sorbonne Université, CNRS, 75005 Paris, France |
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| Abstract: | The Ugi-Smiles reaction of S-benzyl thiouracil have been exploited in several three-step sequences for the preparation of aminopyrimidine libraries with high diversity. After the 4-component coupling, oxidation of the thioether to sulfone is followed by displacement of the latter by various carbon-centered nucleophiles (cyanide, malonate, boronic acids) or amines. The efficiency of the whole sequence was further demonstrated with one-pot procedures. |
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| Keywords: | Ugi-smiles Pyrimidines Sulfone Suzuki reaction |
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