Process for preparing 3-fluoroquinolines
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United States of America Patent
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Jul 8, 2008
Grant Date -
Aug 18, 2005
app pub date -
Nov 10, 2004
filing date -
Nov 17, 2003
priority date (Note) -
Expired
status (Latency Note)
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Abstract
The invention relates to a novel preparation of 3-fluoroquinolines of formula (I) ##STR00001## in which R.sub.1, R.sub.2, R.sub.3 and R.sub.4 represent: a) a fluorine; b) an alkyl optionally substituted with one to three fluorines, with OR.sub.5 in which R.sub.5 is an alkyl, a hydrogen or a hydroxyl-protecting group, or with NR'R'' in which R' and R'' represent an alkyl, a hydrogen or an amino-protecting group; c) OR.sub.6 in which R.sub.6 represents a hydrogen, a phenol-protecting group or an alkyl, optionally substituted with a fluorine, with OR.sub.5 or with NR'R'' as defined above; d) NR'.sub.1R''.sub.1 in which R'.sub.1 and R''.sub.1 have the values of R' et R'' or represent an alkyl substituted with a fluorine, with OR.sub.5 or NR'R'' as defined above; e) CO.sub.2R.sub.a, in which R.sub.a represents hydrogen, alkyl or a carboxyl-protecting group, and also novel intermediate compounds. The quinolines of formula (I) are intermediates useful in the preparation of compounds having antibacterial activity, described in particular in applications WO 02/40474 or WO 02/72572.
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