C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 513/04 (2006.01) A61K 31/496 (2006.01) A61P 31/04 (2006.01) B01D 9/02 (2006.01)
Patent
CA 2523854
The invention aims at providing crystals of 6-fluoro-1-methyl-7-[4-(5-methyl-2- oxo-1,3-dioxolen-4-yl)- methyl-1-piperazinyl]-4-oxo-4H-[1,3]thiazeto[3,2- a]quino- line-3-carboxylic acid acetonitrile solvate (compound B) which are useful as an intermediate for producing preferentially III-type crystals of 6- fluoro-1-methyl-7-[4-(5-methyl-2-oxo -1,3-dioxolen-4-yl)methyl-1-piperazinyl]- 4-oxo-4H-[1,3]- Thiazeto[3,2-a]quinoline-3-carboxylic acid (compound A). Compound B can be preferentially crystallized from acetonitrile by controlling the supersaturation concentration, and desolvation of the crystals of compound B can give III-type crystals of compound A.
L'invention concerne la production de cristaux de 6-fluoro-1-méthyl-7-[4-(5-méthyl-2-oxo-1,3-dioxolène-4-yl)-méthyl-1-piperazinyl]-4-oxo-4H-[1,3]thiazeto[3,2-a]quinoline-3-solvate d'acétonitrile d'acide carboxylique (composé B) qui sont utilisés comme intermédiaire dans la production préférentielle de cristaux de type III de 6-fluoro-1-méthyl-7-[4-(5-méthyl-2-oxo-1,3-dioxolène-4-yl)-méthyl-1-piperazinyl]-4-oxo-4H-[1,3]thiazeto[3,2-a]quinoline-3-acide carboxylique (composé A). Ledit composé B peut être, de préférence, cristallisé à partir d'acétonitrile par régulation de la concentration de supersaturation et, en outre, la dissolution des cristaux du composé B peut engendrer des cristaux de type III du composé A.
Akai Jun
Nishida Hiroshi
Fetherstonhaugh & Co.
Nippon Shinyaku Co. Ltd.
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