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    • 8. 发明申请
    • Novel process for preparing 3-fluoroquinolines
    • 制备3-氟喹啉的新方法
    • US20050182259A1
    • 2005-08-18
    • US10985533
    • 2004-11-10
    • Youssef El-AhmadJean-Pierre LeconteJoel MalpartSerge MignaniStephane MuttiMichel Tabart
    • Youssef El-AhmadJean-Pierre LeconteJoel MalpartSerge MignaniStephane MuttiMichel Tabart
    • C07D215/18C07D215/38C07D215/12
    • C07D215/38C07D215/18Y02P20/55
    • The invention relates to a novel preparation of 3-fluoroquinolines of formula (I) in which R1, R2, R3 and R4 represent: a) a fluorine; b) an alkyl optionally substituted with one to three fluorines, with OR5 in which R5 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) OR6 in which R6 represents a hydrogen, a phenol-protecting group or an alkyl, optionally substituted with a fluorine, with OR5 or with NR′R″ as defined above; d) NR′1R″1 in which R′1 and R″1 have the values of R′ et R″ or represent an alkyl substituted with a fluorine, with OR5 or NR′R″ as defined above; e) CO2Ra, in which Ra 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.
    • 本发明涉及式(I)的3-氟喹啉的新型制备方法,其中R 1,R 2,R 3和R 3, 代表:a)氟; b)任选被一至三个氟取代的烷基,其中R 5是烷基,氢或羟基保护基或NR' 其中R'和R“表示烷基,氢或氨基保护基的”R“ c)OR 6其中R 6表示氢,苯酚保护基或任选被氟取代的烷基,OR 5或N >或如上定义的NR'R“ d)NR'1 R“1其中R'1和R”1 <1的数值为 或者代表被氟取代的烷基,其具有如上定义的OR 5或NR'R“; e)其中R aa代表氢,烷基或羧基保护基,以及新的中间体化合物的CO 2 CO 2。 式(I)的喹啉是可用于制备具有抗菌活性的化合物的中间体,特别在申请WO 02/40474或WO 02/72572中有所描述。