Preparation of phosphinodipeptide analogs as building blocks for pseudopeptides synthesis
Preparation of phosphinodipeptide analogs as building blocks for pseudopeptides synthesis
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DOI：
10.1016/s0022-328x(01)01238-4
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发表时间：
2002-02-01
影响因子：
2.3
通讯作者：
Pirat, JL
中科院分区：
文献类型：
--
作者：
Cristau, HJ;Coulombeau, A;Pirat, JL
本文报道了一种简便、有效、总收率高的膦基二肽的合成方法。这种一锅法可以改变磷原子的α位和/或β位以及氮原子的α位上的取代基，包括次磷酸烷基酯与亚胺的加成。然后在丙烯酸酯上进行迈克尔加成。为了显示膦基二肽类似物I作为合成中间体的价值，描述了三个官能团的选择性脱保护。(C)2002 Elsevier Science B. V.保留所有权利。
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.