公开(公告)号：KR100380322B1

公开(公告)日：2003-04-16

申请号：KR1020000009063

申请日：2000-02-24

Applicant: 한국과학기술연구원

Inventor： 고훈영 ,  최경일 ,  조용서 ,  배애님 ,  차주환 ,  김보형

IPC: C07D501/16

CPC classification number: Y02P20/55

Abstract: PURPOSE: Provided is an isothiazol cephem derivative which has broad range of antimicrobial activity. And its producing method is also provided. CONSTITUTION: The cephalosporin compound represented by formula (1) and its pharmaceutically acceptable salts are produced. In the formula, R1 is hydrogen or an amine protecting group generally used in cephalosporin compound; R2 is hydrogen or an oxim protecting group; R3 is hydrogen or a chloro group; R5 is hydrogen or an ester producing group, a salt producing atom or a carboxy protecting group; and R4 is ring substituent having Q group, in which Q is hydrogen, halogen, hydroxy, mercapto, cyano, carboxy, carboxylic acid ester, carbamoyloxymethyl, N,N-dimethylcarbamoyloxymethyl, carbamoyl, N,N-dimethylcarbamoyl, C1 to C4 alkyl, C1 to C4 alkyloxy, halogen substituted methyl, halogen substituted C1 to C4 alkyloxy, aryl or hetero ring substituent. The cephalosporin derivative of the formula (1) is produced by reacting a compound of formula (7) with a compound of formula (8).

Abstract translation: 目的：提供具有广泛抗微生物活性的异噻唑头孢烯衍生物。 并提供其制作方法。 构成：由式（1）表示的头孢菌素化合物及其药学上可接受的盐被制备。 在该式中，R1是氢或通常用于头孢菌素化合物中的胺保护基; R2是氢或肟保护基; R3是氢或氯基; R5是氢或产酯基团，产盐原子或羧基保护基团; 其中Q为氢，卤素，羟基，巯基，氰基，羧基，羧酸酯，氨基甲酰氧基甲基，N，N-二甲基氨基甲酰氧基甲基，氨基甲酰基，N，N-二甲基氨基甲酰基，C1-C4烷基， C1至C4烷氧基，卤素取代的甲基，卤素取代的C1至C4烷氧基，芳基或杂环取代基。 式（1）的头孢菌素衍生物通过使式（7）的化合物与式（8）的化合物反应来制备。

公开(公告)号：KR1020010084201A

公开(公告)日：2001-09-06

申请号：KR1020000009063

申请日：2000-02-24

Applicant: 한국과학기술연구원

Inventor： 고훈영 ,  최경일 ,  조용서 ,  배애님 ,  차주환 ,  김보형

IPC: C07D501/16

CPC classification number: Y02P20/55

Abstract: PURPOSE: Provided is an isothiazol cephem derivative which has broad range of antimicrobial activity. And its producing method is also provided. CONSTITUTION: The cephalosporin compound represented by formula (1) and its pharmaceutically acceptable salts are produced. In the formula, R1 is hydrogen or an amine protecting group generally used in cephalosporin compound; R2 is hydrogen or an oxim protecting group; R3 is hydrogen or a chloro group; R5 is hydrogen or an ester producing group, a salt producing atom or a carboxy protecting group; and R4 is ring substituent having Q group, in which Q is hydrogen, halogen, hydroxy, mercapto, cyano, carboxy, carboxylic acid ester, carbamoyloxymethyl, N,N-dimethylcarbamoyloxymethyl, carbamoyl, N,N-dimethylcarbamoyl, C1 to C4 alkyl, C1 to C4 alkyloxy, halogen substituted methyl, halogen substituted C1 to C4 alkyloxy, aryl or hetero ring substituent. The cephalosporin derivative of the formula (1) is produced by reacting a compound of formula (7) with a compound of formula (8).

Abstract translation: 目的：提供具有广泛抗菌活性的异噻唑头孢烯衍生物。 并提供其生产方法。 构成：制备由式（1）表示的头孢菌素化合物及其药学上可接受的盐。 在该式中，R 1是氢或通常用于头孢菌素化合物中的胺保护基; R2是氢或肟基保护基; R3是氢或氯基; R5是氢或产酯基，产盐原子或羧基保护基; R4是具有Q基团的环取代基，其中Q是氢，卤素，羟基，巯基，氰基，羧基，羧酸酯，氨基甲酰氧基甲基，N，N-二甲基氨基甲酰氧基甲基，氨基甲酰基，N，N-二甲基氨基甲酰基， C1至C4烷氧基，卤素取代的甲基，卤素取代的C1至C4烷氧基，芳基或杂环取代基。 式（1）的头孢菌素衍生物通过使式（7）的化合物与式（8）的化合物反应来制备。