Preparation of phosphinodipeptide analogs as building blocks for pseudopeptides synthesis
作者:Henri-Jean Cristau、Agnès Coulombeau、Arielle Genevois-Borella、Frédéric Sanchez、Jean-Luc Pirat
DOI:10.1016/s0022-328x(01)01238-4
日期:2002.2
A simple and effective preparation of phosphinodipeptides, in good overall yields, has been developed, This one pot procedure, allowing the variation of the substituents in alpha and/or beta position to the phosphorus atom and also in alpha position to the nitrogen atom, consists in the addition of alkyl hypophosphites to imines. followed by Michael-addition on acrylates. To show the value of phosphinodipeptides analogs I as synthetic intermediates, selective deprotections of the three functional groups are described. (C) 2002 Elsevier Science B.V. All rights reserved.