Publication number: 20070208174
Abstract: A process for the preparation of the boron difluoride chelate of quinolone-3-carboxylic acid of formula I, where R1 is an optionally substituted C1-5 alkyl, an optionally substituted C3-6 cycloalkyl, or aryl; R2 is a C1-5 alkyl, alkoxy, amino, alkylamino, or acylamino; R3 is a hydrogen, halogen, C1-5 alkoxy, amino, alkylamino, or acylamino; or when R3 is O or S forms an optionally substituted 5-, 6- or 7-membered ring T with R1, or if the ring T is substituted, the substituent is an optionally substituted C1-5 alkyl, an optionally substituted C3-6 cycloalkyl, or aryl; X is hydrogen, chloride or fluoride; and Y is chloride or fluoride; via: (a) the reaction of quinolone-3-carboxylic acid derivative II, where R1, R2, R3, T, X, and Y are as defined above and R4 is hydrogen, optionally substituted C1-5 alkyl, optionally subsituted C3-6 cycloalkyl, alkylsilyl, aryl or arylalkyl, with: (b) fluoroboric acid or trifluoroborane in the presence of a silicon-containing compound, wherein the silicon-containin
Type:
Application
Filed:
March 2, 2006
Publication date:
September 6, 2007
Inventors:
Zhi-Xian Wang, Murali Kondamreddy, Joseph DiMartino, Bhaskar Guntoori