Novel synthesis of 3,4-dihydro-5-bromo[1,4]oxazin-2-one derivatives, new protease inhibitor scaffold

被引：29

作者：

Bihel, F ^{[1
]}

Kraus, JL ^{[1
]}

机构：

[1] Univ Mediterranee AP Marseille, Fac Sci Luminy, INSERM, U382,Dev Biol Inst Marseille,Lab Chim Biomol,CNRS, F-13288 Marseille 09, France

来源：

ORGANIC & BIOMOLECULAR CHEMISTRY | 2003年 / 1卷 / 05期

关键词：

D O I：

10.1039/b212064j

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

We designed and synthesized a new class of serine protease inhibitors based on the oxazinone core. To this end, we first developed a short and efficient route to synthesize a new 3,4-dihydro[1,4]oxazin-2-one ring. Then we successfully synthesised the corresponding 5-bromo derivatives which have never been reported before, and demonstrated their inhibitory activities on a-chymotrypsin.

引用

页码：793 / 799

页数：7

共 20 条

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[2]

BIHEL F, 2002, Patent No. 0248102

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