Sesquihydrate of naphthyridine derivatives, and process for...

C - Chemistry – Metallurgy – 07 – D

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C07D 471/04 (2006.01) C07D 213/73 (2006.01) C07D 213/74 (2006.01) C07D 213/75 (2006.01) C07D 213/77 (2006.01)

Patent

CA 1216292

Abstract of the Disclosure Novel l-ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(1- piperazinyl)-1,8-naphthyridine-3-carboxylic acid.sesqui- hydrate (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 enough to form the sesquihydrate. This sesqui- hydrate 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 pharma- ceutical compound.

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