110548-07-7Relevant articles and documents
Asymmetric metal-free synthesis of fluoroquinolones by organocatalytic hydrogenation
Rueping, Magnus,Stoeckel, Mirjam,Sugiono, Erli,Theissmann, Thomas
experimental part, p. 6565 - 6568 (2010/10/19)
A highly enantioselective organocatalytic transfer hydrogenation enabling the synthesis of both 6-fluoro-2-methyltetrahydroquinoline and 7,8-difluoro-3-methyl-benzoxazine has been developed. These key building blocks can for the first time be synthesized using the same methodology allowing fast and efficient, metal-free access to the antibiotic fluoroquinolones flumequine and levofloxacine.
Optically active benzoxazines and bezothiazines and a process for their stereospecific preparation
-
, (2008/06/13)
Optically active 7,8-difluoro-3,4-dihydro-3--methyl-2H-[1,4]benzoxazines and 7,8-difluoro-3,4-dihydro-2--methyl-2H-[1,4]benzoxazines and the corresponding benzothiazines of formula III, where, one of the substituents R1, R2, R3 and R4 is CH2OH or -CH2Z, the remaining being hydrogen, X denotes fluoro, chloro, methyl or hydrogen, Y is oxygen or sulfur and Z is hydrogen, fluoro or protected hydroxyl are obtained as the stereochemically pure products of a stereospecific synthesis using a 3,4-difluoronitrobenzene substituted with a stereochemically pure 2-(1-hydroxyisopropoxy), 2-(2--hydroxypropoxy), 2-(1-hydroxyisopropylthio) or 2-(2--hydroxypropylthio) substituent. The obtained compounds are suited for the production of optically active pyridobenzoxazines and pyridobenzothiazines, among which are useful antibacterial optically active quinolones, particularly (S)-(-)-ofloxacin.
Synthesis and antibacterial activities of optically active ofloxacin and its fluoromethyl derivative.
Atarashi,Yokohama,Yamazaki,Sakano,Imamura,Hayakawa
, p. 1896 - 1902 (2007/10/02)
-
