References of 7-(3-aminopyrrolidin-1-yl)-1-(2,4-difluorophenyl)-6-fluoro-4-oxo-1,
8-naphthyridine-3-carboxylic acid
Title: Tosufloxacin
CAS Registry Number: 100490-36-6
CAS Name: 7-(3-Amino-1-pyrrolidinyl)-1-(2,4-difluorophenyl)-6-fluoro-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid
Manufacturers' Codes: A-61827
Molecular Formula: C19H15F3N4O3
Molecular Weight: 404.34
Percent Composition: C 56.44%, H 3.74%, F 14.10%, N 13.86%, O 11.87%
Literature References: Trifluorinated quinolone antibacterial. Prepn: H. Narita
et al., DE 3514076 (1985 to Toyama),
C.A. 104, 129888r (1986); D. T. W. Chu,
EP 153580;
idem, US 4616019 (1985, 1986 both to Abbott); and activity:
idem et al., J. Med. Chem. 29, 2363 (1986); H. Narita
et al., Yakugaku Zasshi 106, 802 (1986),
C.A. 106, 196291v (1987).
In vitro activity studies of the base: P. B. Fernandes
et al., Antimicrob. Agents Chemother. 32, 27 (1988); and
in vivo animal studies of the toluenesulfonate: M. Takahata
et al., J. Antimicrob. Chemother. 22, 143 (1988). Series of articles on antibacterial activity and clinical evaluation:
Chemotherapy (Tokyo) 36, Suppl. 9, 1-1538 (1988).
Derivative Type: Hydrochloride
CAS Registry Number: 104051-69-6
Manufacturers' Codes: A-60969
Molecular Formula: C19H15F3N4O3.HCl
Molecular Weight: 440.80
Percent Composition: C 51.77%, H 3.66%, F 12.93%, N 12.71%, O 10.89%, Cl 8.04%
Properties: Crystals from conc HCl-ethanol (1:3), mp 247-250° (dec).
Melting point: mp 247-250° (dec)
Derivative Type: Toluenesulfonate
CAS Registry Number: 115964-29-9
Synonyms: Tosufloxacin tosylate
Manufacturers' Codes: A-64730; T-3262
Trademarks: Ozex (Toyama); Tosuxacin (Dainabot)
Molecular Formula: C19H15F3N4O3.C7H8O3S
Molecular Weight: 576.54
Percent Composition: C 54.16%, H 4.02%, F 9.89%, N 9.72%, O 16.65%, S 5.56%
Properties: Prepd as the monohydrate, mp 258-260°.
Melting point: mp 258-260°
Therap-Cat: Antibacterial.
Keywords: Antibacterial (Synthetic); Quinolones and Analogs.
