Novel Approach for the Synthesis of Five-Membered-Ring-Fused Pyrazinones

被引：5

作者：

Gembus, Vincent ^{[1
]}

Janvier, Solenn ^{[2
]}

Lecouve, Jean-Pierre ^{[2
]}

Gloanec, Philippe ^{[3
]}

Marsais, Francis ^{[1
]}

Levacher, Vincent ^{[1
]}

机构：

[1] Univ Rouen, IRCOF, Associe CNRS, COBRA,UMR 6014,INSA, F-76130 Mont St Aignan, France

[2] Oril Ind, F-76210 Bolbec, France

[3] Inst Rech Servier, F-92150 Suresnes, France

来源：

EUROPEAN JOURNAL OF ORGANIC CHEMISTRY | 2010年 / 2010卷 / 19期

关键词：

Alkylation; Heterocycles; Peptidomimetics; Pyrazinones; Serine protease inhibitor; INHIBITORS; DESIGN; POTENT;

D O I：

10.1002/ejoc.201000435

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

We describe a new route to access important pharmaceutical intermediates for the synthesis of constrained fused pyrazinones. These compounds are prepared in five to seven steps with a good overall yield from glycine methyl ester and commercial propanediol derivatives involving an intramolecular alkylation of a glycine moiety as key step.

引用

页码：3583 / 3586

页数：4

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