KR940002240A - Quinolone and naphthyridine carboxylic acid derivatives and preparation method thereof - Google Patents

Quinolone and naphthyridine carboxylic acid derivatives and preparation method thereof Download PDF

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KR940002240A
KR940002240A KR1019920012656A KR920012656A KR940002240A KR 940002240 A KR940002240 A KR 940002240A KR 1019920012656 A KR1019920012656 A KR 1019920012656A KR 920012656 A KR920012656 A KR 920012656A KR 940002240 A KR940002240 A KR 940002240A
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South Korea
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group
general formula
hydrogen
following general
compound represented
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KR1019920012656A
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Korean (ko)
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서귀현
장만식
김정환
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김생기
영진약품공업 주식회사
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Publication of KR940002240A publication Critical patent/KR940002240A/en

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Abstract

본 발명은 우수한 항균활성을 나타내는 다음 구조식(Ⅰ)의 신규한 퀴놀론 및 나프티리딘 카르복실산 유도체와 그 제조방법에 관한 것이다.The present invention relates to novel quinolone and naphthyridine carboxylic acid derivatives of the following structural formula (I) exhibiting excellent antimicrobial activity and methods for their preparation.

상기식에서 R1은 에틸, 2-플루오로에틸, 2,2,2,-트리플루오로에틸, 시클로프로필, tert-부틸, 4-플루오로 페닐 또는 2,4-디플루오로페닐 기이고; R2는 수소 또는 아미노 기이며; R3는 수소 또는 메틸 기이고; X는 CH, CF 또는 N이고; Y는 포르밀, 포름이미도일, 아세트이미도일, 아미디노 기이다.R 1 is an ethyl, 2-fluoroethyl, 2,2,2, -trifluoroethyl, cyclopropyl, tert-butyl, 4-fluoro phenyl or 2,4-difluorophenyl group; R 2 is hydrogen or an amino group; R 3 is hydrogen or a methyl group; X is CH, CF or N; Y is a formyl, formimidoyl, acetimidoyl, amidino group.

Description

퀴놀론 및 나프티리딘 카르복실산 유도체와 그 제조방법Quinolone and naphthyridine carboxylic acid derivatives and preparation method thereof

본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음Since this is an open matter, no full text was included.

Claims (4)

다음 일반식 (Ⅰ)로 표시되는 화합물과 약학적으로 허용가능한 그의 염The compound represented by the following general formula (I) and a pharmaceutically acceptable salt thereof 상기식에서 R1은 에틸, 2-플루오로에틸, 2,2,2,-트리플루오로에틸, 시클로프로필, tert-부틸, 4-플루오로 페닐 또는 2,4-디플루오로페닐 기이고; R2는 수소 또는 아미노 기이며; R3는 수소 또는 메틸 기이고; X는 CH, CF 또는 N이고; Y는 포르밀, 포름이미도일, 아세트이미도일, 아미디노 기이다.R 1 is an ethyl, 2-fluoroethyl, 2,2,2, -trifluoroethyl, cyclopropyl, tert-butyl, 4-fluoro phenyl or 2,4-difluorophenyl group; R 2 is hydrogen or an amino group; R 3 is hydrogen or a methyl group; X is CH, CF or N; Y is a formyl, formimidoyl, acetimidoyl, amidino group. 제1항에 있어서, 임반식(I)의 R1은 에틸, 2-플루오로에틸, 2,2,2,-트리플루오로에틸, 시클로프로필, tert-부틸, 4-플루오로페닐 또는 2,4-디플루오로 페닐 기이고; R2는 수소 또는 아미노 기이며; R3는 수소 또는 메틸 기이고; X는 CH, CF 또는 N이고; Y는 포름이미도일 기인 것을 특징으로 하는 일반식(Ⅰ)로 표시되는 화합물과 약학적으로 허용가능한 그의 염.The compound of claim 1, wherein R 1 in the general formula (I) is ethyl, 2-fluoroethyl, 2,2,2, -trifluoroethyl, cyclopropyl, tert-butyl, 4-fluorophenyl or 2, 4-difluoro phenyl group; R 2 is hydrogen or an amino group; R 3 is hydrogen or a methyl group; X is CH, CF or N; Y is a compound represented by the general formula (I), and a pharmaceutically acceptable salt thereof, characterized in that it is a formimidoyl group. 다음 일반식(Ⅱ)로 표시되는 화합물과 다음 일반식(Ⅲ)로 표시되는 화합물을 반응시켜서 되는 것을 특징으로 하는 다음 일반식(Ⅰ)로 표시되는 퀴놀론 나프티리딘카르복실산 유도체의 제조방법.A method for producing a quinolone naphthyridine carboxylic acid derivative represented by the following general formula (I), which comprises reacting a compound represented by the following general formula (II) with a compound represented by the following general formula (III). 상기식에서, R1,R2,R3,X 및 Y는 앞에서 정의한 바와 같고 R4는 수소 또는 제거가 가능한 보호기이며, R5는 수소, 메틸 및 메틸티오 그룹이고, R6는 아미노 및 에톡시 그룹, X'는 클로, 하이드로설페이트, 요오드 및 아세테이트 이온을 나타낸다.Wherein R 1 , R 2 , R 3 , X and Y are as defined above and R 4 is hydrogen or a removable protecting group, R 5 is hydrogen, methyl and methylthio group, and R 6 is amino and ethoxy Group, X ′ represents claw, hydrosulfate, iodine and acetate ions. 다음 일반식(Ⅳ)로 표시되는 화합물과 다음 일반식(Ⅴ)으로 표시되는 화합물을 반응시켜서 되는 것을 특징으로 하는 다음 일반식(Ⅰ)으로 표시되는 퀴놀론 및 나프티리딘 카르복실산 유도체의 제조방법.A process for producing a quinolones and naphthyridine carboxylic acid derivatives represented by the following general formula (I) characterized by reacting a compound represented by the following general formula (IV) with a compound represented by the following general formula (V). 상기식에서, R1,R2,R3,X 및 Y는 앞에서 정의한 바와 같고 -R4는 수소 또는 제거가 가능한 보호기이며, Z는 클로로 또는 플루오로 기를 나타낸다.Wherein R 1 , R 2 , R 3 , X and Y are as defined above and -R 4 is hydrogen or a removable protecting group and Z represents a chloro or fluoro group. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.※ Note: The disclosure is based on the initial application.
KR1019920012656A 1992-07-16 1992-07-16 Quinolone and naphthyridine carboxylic acid derivatives and preparation method thereof KR940002240A (en)

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