Generated: May 23, 2017
|Title:||8-alkoxyquinolonecarboxylic acid hydrate with excellent stability and process for producing the same|
|Abstract:||The invention provides 1-cyclopropyl-6-fluoro-1,4- dihydro-8-methoxy-7-(3-methyl-1-piperazinyl)-4-oxo-3- quinolinecarboxylic acid sesquihydrate with excellent stability represented by a following formula (1), ##STR1## and process for producing the same.|
|Inventor(s):||Matsumoto; Toyomi (Kamiina-gun, JP), Hara; Masamoto (Okaya, JP), Miyashita; Kunio (Okaya, JP), Kato; Yukihiro (Okaya, JP)|
|Assignee:||Kyorin Pharmaceutical Co., Ltd. (Tokyo, JP)|
1. 1-Cyclopropyl-6- fluoro-1,4-dihydro-8-methoxy-7-(3-methyl-1-piperazinyl)-4-oxo-3-quinolineca rboxylic acid sesquihydrate represented by a formula (1) ##STR4##
2. A process for producing the compound of claim 1, characterized in that an aqueous suspension of 1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-(3-methyl-1-piperazinyl)-4- oxo-3-quinolinecarboxylic acid is treated by heating under stirring.
3. The process of claim 2 wherein said aqueous suspension is heated at a temperature of 50.degree. to 100.degree. C.
4. The process of claim 3 wherein said temperature is 80.degree. to 90.degree. C.
5. The process of claim 2 wherein said aqueous suspension is at a pH in the range 6.0 to 8.0.
6. The process of claim 2 wherein said suspension is hot filtered at the same temperature at which it is treated.
7. The process of claim 6 wherein, after collecting a first crop of crystals, a second crop is obtained by cooling the filtrate to room temperature.
8. The process of claim 3 wherein, after collecting a first crop of crystals, a second crop is obtained by cooling the filtrate to room temperature.
9. The process of claim 2 wherein said aqueous suspension is the suspension obtained after neutralization in the acid-alkali recrystallization during the process of purifying said 1-cyclopropyl-6-fluoro-1,4 dihydro-8-methoxy-7-(3-methyl-1-piperazinyl)-4-oxo-3-quinoline carboxylic acid.
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