| 摘要 |
<p>1362839 Preparation of 5-fluorouracils RESEARCH INSTITUTE FOR MEDICINE & CHEMISTRY Inc 4 Oct 1971 [5 Oct 1970] 46100/71 Heading C2C 5-Fluoro-uracils of the formula wherein R<SP>1</SP> and R<SP>3</SP> are the same or different and are alkyl or hydrogen and R<SP>2</SP> is alkyl, hydrogen or a sugar residue are prepared by the reactionof uracils of the Formula II with a hypofluorite the fluoroxy group of which is covalently bonded to an inert electron attracting group or with elemental fluorine diluted with an inert gas and decomposition of the intermediates so formed for example by heating. One intermediate formed is the novel 5-fluoro-6- hydroxy-5,6-dihydro-uracil which is characterized by an Rf value of 0À3 for thin layer chromatography on silica gel using methanol : chloroform (20 : 80) as eluant, an infra-red spectrum with absorption maxima (KBr disc) at 3300, 1720, 1475, 1250, 1140, 1080, 880 and 800 cm<SP>-1</SP>, a PMR spectrum comprising a complex pattern of resonances from 5-6 p.p.m. which is characteristic of the AB pattern of an ABX system and an FMR spectrum comprising a signal at # + 207À6 p.p.m. which is a broad doublet with J = 45 Hz. The products of the above process have cytotoxic properties.</p> |
