- NOVEL METHOD OF SYNTHESIS OF FLUOROQUINOLONES
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The invention relates to a method of preparation of fluoroquinolones of formula (I) from compounds of formula (II): in which R1, R2, R3, R4, R5, R6, R7, and X are as defined in Claim 1.
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Page/Page column 6; 9
(2009/04/24)
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- Sesquihydrate of naphthyridine derivative, and process for the preparation thereof
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Novel 1-ethyl-6-fluoro-1,4-dihyono-4-oxo -7-(1-piperazinyl)-1,8-naphthyridine-3-carboxylic acid.sesquihydrate (ATT-2266.sesquihydrate). The aforesaid compound can be prepared by heating 1-ethyl-6-fluoro-1,4-dihydro-4-oxo -7-(1-piperazinyl)-1,8-naphthyridine-3-carboxylic acid at a temperature above about 60° C. in the presence of water in an amount sufficient to form the sesquihydrate. This sesquihydrate is much more stable than the anhydrate and the trihydrate and is superior to the anhydrate in the rate of dissolution and transference into the body through the intestines. Thus, it is especially useful as a pharmaceutical compound.
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- Novel naphthyridine derivatives, intermediates thereof, processes for preparation thereof, and use thereof
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This invention relates to 1,8-naphthyridine compounds of the formula STR1 wherein X is a halogen atom especially fluorine atom, R1 is an ethyl group or a vinyl group, and R2 is a hydrogen atom or a lower alkyl group, their salts and processes for the preparation of them. The 1,8-naphthyridine compounds and their salts are useful as antibacterial agents and intermediates thereof.
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