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A convenient one-pot synthesis of phosphino-dipeptide analogs

✍ Scribed by Henri-Jean Cristau; Agnès Coulombeau; Arielle Genevois-Borella; Jean-Luc Pirat

Publisher
Elsevier Science
Year
2001
Tongue
French
Weight
97 KB
Volume
42
Category
Article
ISSN
0040-4039

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✦ Synopsis

A general one-pot synthesis is described for the preparation, in good overall yields, of phosphinopeptides as building blocks for peptide synthesis in the field of new enzyme inhibitors. This method, consisting of the addition of alkyl hypophosphites to imines and then in the Michael-addition of the resulting alkyl a-aminophosphonites on acrylates, affords the possibility of variations for the substituents in a and b position to the phosphorus atom and in a position to the nitrogen atom.

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