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|Title:||7-(4-aminomethyl-3-me thyloxyiminopyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8 -naphthyridine-3-carboxylic acid and the process for the preparation thereof|
|Abstract:||The present invention relates to a novel quinolone compound having an excellent antibacterial activity. More specifically, the present invention relates to 7-(4-aminomethyl-3-methyloxyiminopyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4 -oxo-1,4-dihydro-1,8-naphthyridine -3-carboxylic acid represent by the following formula: ##STR1## or its isomer.|
|Inventor(s):||Hong; Chang Yong (Daejon, KR), Kim; Young Kwan (Daejon, KR), Kim; Se Ho (Daejon, KR), Chang; Jay Hyok (Daejon, KR), Choi; Hoon (Daejon, KR), Nam; Do Hyun (Daejon, KR), Kim; Ae Ri (Daejon, KR), Lee; Jin Hwa (Daejon, KR), Park; Ki Sook (Daejon, KR)|
|Assignee:||LG Chemical Ltd. (Seoul, KR)|
|Filing Date:||Mar 27, 1998|
|Claims:||1. A process for preparing 7-(4-aminomethyl-3-methyloxyiminopyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4 -oxo-1,4-dihydro-1,8-naphthyridine- 3-carboxylic acid represented by the following formula: ##STR271## or its isomer, methanesulfonate and hydrate of the methanesulfonate, which comprises reacting a quinolone compound represented by the following formula, ##STR272## in which X represents a halogen, with a protected pyrrolidine oxime compound represented by the following formula, ##STR273## in which P represents an amino-protecting group, in the presence of a base and then removing the amino-protecting group P from the resulting compound. |
2. The process of claim 1, wherein the amino-protecting group is selected from the group consisting of formyl, acetyl, trifluoroacetyl, benzoyl, para-nitrobenzoyl, para-toluenesulfonyl, methoxycarbonyl, ethoxycarbonyl, t-butoxycarbonyl, benzyloxycarbonyl, para-methoxybenzyloxycarbonyl, trichloroethoxycarbonyl, benzyl, para-methoxybenzyl, trityl and tetrahydropyranyl.
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