PREPARATION AND BIOLOGICAL EVALUATION OF A-FLUOROMETHYL-ALPHA-METHYLENE-GAMMA-BUTYROLACTONE AND GAMMA-BUTYROLACTAM

Authors
MURATA K KANEKO S KITAZUME T
Citation
K. Murata et al., PREPARATION AND BIOLOGICAL EVALUATION OF A-FLUOROMETHYL-ALPHA-METHYLENE-GAMMA-BUTYROLACTONE AND GAMMA-BUTYROLACTAM, Bioorganic & medicinal chemistry letters, 3(12), 1993, pp. 2685-2688
Citations number
8
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
3
Issue
12
Year of publication
1993
Pages
2685 - 2688
Database
ISI
SICI code
0960-894X(1993)3:12<2685:PABEOA>2.0.ZU;2-F
Abstract
Difluoromethyl-alpha-methylene-gamma-butyrolactone 2 was readily prepa red from the Reformatsky-type reaction of difluoroacetaldehyde ethyl h emiacetal 1 and methyl 2-(bromomethyl)acrylate in Zn-THF system, and d ifluoromethyl-alpha-methylene-gamma-butyrolactams 6 were also prepared from difluoroethanimine. Difluoromethyl-alpha-methylene-gamma-butyrol actone 2 was found to possess comparable or even stronger in vitro ant itumoral activity than the currently used 5-fluorouracil.