| 摘要 |
<p>Preparation of 3-fluoro-quinolines (I) (optionally substituted in the 5-, 6-, 7- and/or 8-position) involves heating a corresponding quinoline-3-diazonium tetrafluoroborate (II) in an inert organic solvent. Preparation of 3-fluoro-quinolines of formula (I) involves heating a quinoline-3-diazonium tetrafluoroborate of formula (II) in an inert organic solvent. [Image] R 1 - R 4H or F; linear, branched or cyclic alkyl (optionally substituted by 1-3 F, by OR 5 or by NR'R''); OR 6, NR' 1R'' 1 or COOR a; or phenyl or heteroaryl, both optionally substituted by one or more of the substituents given above or below; R 5H, alkyl or hydroxy-protecting group; R', R'' : H, alkyl or amino-protecting group; R 6H, phenol protecting group or alkyl (optionally substituted by 1-3 F, by OR 5 or by NR'R''); R' 1, R'' 1as for R', R''; or alkyl substituted by 1-3 F, by OR 5 or by NR'R''; and R aH, alkyl or carboxy-protecting group. An independent claim is included for (II) as new compounds.</p> |
