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Ugi reaction for the synthesis of 4-aminopiperidine-4-carboxylic acid derivatives. Application to the synthesis of carfentanil and remifentanil
Authors:Sandra Malaquin  Guillaume Laconde
Affiliation:Biostructures and Drug Discovery, INSERM U761, Faculté de Pharmacie, Université Lille Nord de France, Lille F-59006, France PRIM Pôle de Recherche Interdisciplinaire sur le Médicament, Lille F-59000, France
Abstract:A two-step sequence involving an Ugi four-component reaction was developed for the preparation of 4-aminopiperidine-4-carboxylic acid derivatives. This strategy has led to the successful preparation of two drugs carfentanil and remifentanil in shorter times and better yields than previously described methods.
Keywords:Ugi reaction   Remifentanil   Carfentanil   Mumm rearrangement
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