Synthesis of 2-methyl-5-amino-4-oxo-3-sulfonyl esters as precursors of pseudodipeptides

被引：0

作者：

Severi D. ^{[1
]}

Ettouati L. ^{[1
]}

Paris J. ^{[1
]}

机构：

[1] Universite Claude Bernard Lyon 1, Inst. des Sci. Pharmaceut./Biol., Lab. de Chim. Therapeutique EA 635, F-69373 Lyon Cedex 08

来源：

Letters in Peptide Science | 2002年 / 9卷 / 1期

关键词：

β-ketosulfone; 2-methyl-5-amino-4-oxo-3-sulfonyl esters; Carba isostere; E-alkene isostere; Ketomethylene isostere;

D O I：

10.1023/A:1021355216656

中图分类号：

学科分类号：

摘要：

The synthesis of 2-methyl-5-amino-4-oxo-3-sulfonyl esters, potential precursors of Xaaψ[COCH2]Ala, Xaaψ[E-CH=CH]Ala and Xaaψ[CH2CH2]Ala pseudodipeptides, has been investigated by alkylation of aminoacid-derived β-ketosulfones with ethyl 2-bromo- or 2-triflyloxypropionate in different basic conditions. Yields in 2-methyl-5-amino-4-oxo-3-sulfonyl esters are low but starting β-ketosulfones are recovered in good yield.

引用

页码：11 / 14

页数：3

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