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
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
收藏
页码:3583 / 3586
页数:4
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