3,6-DIOXOPERHYDROPYRROLO[1,2-A]PYRAZINES - A NEW APPROACH TO CONFORMATIONALLY RESTRICTED TRIPEPTIDES

被引：8

作者：

MARTINMARTINEZ, M ^{[1
]}

GARCIALOPEZ, MT ^{[1
]}

GONZALEZMUNIZ, R ^{[1
]}

机构：

[1] INST QUIM MED,JUAN CIERVA 3,E-28006 MADRID,SPAIN

来源：

TETRAHEDRON LETTERS | 1992年 / 33卷 / 16期

关键词：

D O I：

10.1016/0040-4039(92)88173-3

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Catalytic hydrogenation of the 4-ketodiesters, obtained from Z-Xaa-Gly (Xaa = Ala, Phe) halomethyl ketones and dimethyl malonate, provides readily access to the corresponding 4-substituted-3,6-dioxoperhydropyrrolo[1,2-a]pyrazine-7-carboxylic acid derivatives with high degree of stereocontrol at the new chiral centers. Alkylation of these bicyclic bis-lactams with benzyl bromide gave the corresponding Xaa-Gly-Phe restricted tripeptides.

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页码：2187 / 2190

页数：4

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