SYNTHESIS AND ANTIBACTERIAL ACTIVITY OF 2,3-DEHYDROOFLOXACIN

被引：10

作者：

AUGERI, DJ

FRAY, AH

KLEINMAN, EF

机构：

[1] Pfizer Central Research, Groton, Connecticut

来源：

JOURNAL OF HETEROCYCLIC CHEMISTRY | 1990年 / 27卷 / 05期

关键词：

D O I：

10.1002/jhet.5570270561

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

The 2,3‐dehydro analog 2 of the potent quinolone antibacterial agent ofloxacin (1) was synthesized by an efficient six step route beginning with ethyl 2,3,4,5‐tetrafluorobenzoylacetate. Formation of the oxazine ring of 2 was accomplished by ozonolysis of 1‐(1‐buten‐3‐yl)quinolone 5 to the corresponding aldehyde, which cyclized upon treatment with base via intramolecular displacement of the C‐8 fluorine to afford tricyclic ester 6. The antibacterial activities of 2,3‐dehydroofloxacin (2) and ofloxacin (1) are compared. Copyright © 1990 Journal of Heterocyclic Chemistry

引用

页码：1509 / 1511

页数：3

共 10 条

[1]

CHU DT, 1985, Patent No. 4533663

[2] SYNTHESIS OF 4-OXO-4H-QUINO[2,3,4-I,J][1,4]-BENOXAZINE-5-CARBOXYLIC ACID-DERIVATIVES [J].