Regioselective two step synthesis of 3-substituted 2-aminoimidazo[1,2-a]pyrimidines |
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Authors: | Santiago Carballares Marta M Cifuentes |
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Institution: | a Departamento de Investigación, Lilly, S.A. Avda. de la Industria, 30, 28108 Alcobendas, Madrid, Spain b X-ray Crystallography, Eli Lilly and Company, Indianapolis, IN 46285, USA |
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Abstract: | A two step procedure for the regioselective synthesis of 3-substituted-2-aminoimidazo1,2-a]pyrimidines is described. The key step is a Dimroth rearrangement of a mixture of 2 and 3-substituted aminoimidazo1,2-a]pyrimidines that yields quantitatively one regioisomer. Reaction screening for the rearrangement step is reported. A multicomponent isocyanide based reaction is chosen as the preferred way for the synthesis of the precursors. Elucidation of regiochemistry has been done by X-ray determination of some representative compounds. |
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