公开(公告)号：KR100333492B1

公开(公告)日：2002-04-25

申请号：KR1019990019241

申请日：1999-05-27

Applicant: 한국과학기술연구원

Inventor： 고훈영 ,  장문호 ,  조영서 ,  최경일 ,  배애님 ,  김혜연 ,  주현진

IPC: C07D413/14

Abstract: 일반식(II)로표시되는옥사졸리디논유도체와일반식(III)으로표시되는이소옥사졸유도체를용매와환원제존재하에반응시켜 MRSA 균주를포함한그람양성균에우수한신규의일반식 (I)로표시되는이소옥사졸릴메틸렌옥사졸리디논유도체및 이의제조방법에관한것이다. 상기식들중, R은수소, 알킬, 브롬또는염소의할로겐, 시아노, 알콜시, 히드록시, 카르복시, 카르바모일, N,N'-디메틸카르바모일, 카르바모일옥시, 산소, 황, 질소원자를적어도한 개이상포함하고있는티오펜, 티아졸, 아미노티아졸, 이소티아졸, 이소옥사졸, 옥사졸, 테트라졸, 피리딘의불포화 5환또는 6환헤테로고리치환체, 알킬, 할로겐알콕시, 시아노또는페녹시가치환된벤젠고리치환체, 약제학적으로허용되는염의메탄설폰산염, 퓨마렌산염, 브롬산염, 시트릭산염, 인산염, 황산염, 염산염또는염이아닌아민을포함한다.

公开(公告)号：KR1020000074954A

公开(公告)日：2000-12-15

申请号：KR1019990019241

申请日：1999-05-27

Applicant: 한국과학기술연구원

Inventor： 고훈영 ,  장문호 ,  조영서 ,  최경일 ,  배애님 ,  김혜연 ,  주현진

IPC: C07D413/14

Abstract: PURPOSE: Provided is an isooxazolyl methylene oxazolidinone derivative represented by the formula (I) which is superior in antibacterial activity. Also, a method for preparing the compound is provided. CONSTITUTION: An isooxazoly methylene oxazolidinone derivative is represented by the formula (I): wherein, R is hydrogen, alkyl, halogen such as bromine or chlorine, cyano, alkoxy, hydroxy, carboxy, carbamoyl, N,N'-dimethylcarbamoyl, carbamoyloxy, oxygen, sulfur, thiopene having more than one nitrogen atom, thiazole, aminothiazole, isothiazole, isooxazole, oxazole, tetrazole, 5 or 6-membered unsaturated heterocycle substituent of pyridine, alkyl, halogenalkoxy, benzene ring substituted with cyano or phenoxy group, pharmaceutically acceptable methanesulfonate, fumarate, bromate, citrate, phosphate, sulfate or amine not being salt. The isooxazoly methylene oxazolidinone derivative is prepared by reacting oxazolidine derivative represented by the formula (II) and isooxazole derivative represented by the formula (III) a using a reductant in the presence of a solvent.

Abstract translation: 目的：提供抗菌活性优异的由式（I）表示的异恶唑基亚甲基恶唑烷酮衍生物。 此外，提供了制备该化合物的方法。 构型：异恶唑基亚甲基恶唑烷酮衍生物由式（I）表示：其中R是氢，烷基，卤素如溴或氯，氰基，烷氧基，羟基，羧基，氨基甲酰基，N，N'-二甲基氨基甲酰基，氨基甲酰氧基， 氧，硫，具有多于一个氮原子的噻吩，噻唑，氨基噻唑，异噻唑，异恶唑，恶唑，四唑，吡啶，烷基，卤代烷氧基，被氰基或苯氧基取代的苯环的5或6元不饱和杂环取代基， 甲磺酸盐，富马酸盐，溴酸盐，柠檬酸盐，磷酸盐，硫酸盐或胺不是盐。 异恶唑亚甲基恶唑烷酮衍生物通过使用还原剂在溶剂存在下使式（II）表示的恶唑烷衍生物和由式（III）a表示的异恶唑衍生物反应来制备。

公开(公告)号：KR100333493B1

公开(公告)日：2002-04-25

申请号：KR1019990019242

申请日：1999-05-27

Applicant: 한국과학기술연구원

Inventor： 고훈영 ,  장문호 ,  조영서 ,  최경일 ,  배애님 ,  김혜연 ,  주현진

IPC: C07D413/14

Abstract: 일반식(II)로표시되는옥사졸리디논유도체와일반식(III)으로표시되는카르복실산유도체를활성화제, 염기및 용매존재하에아실화반응시켜 MRSA 균주를포함한그람양성균에우수한신규의일반식 (I)로표시되는이소옥사졸릴카르보닐옥사졸리디논유도체및 이의제조방법에관한것이다. 상기식들중, R은수소, 알킬, 브롬또는염소의할로겐, 시아노, 알콕시, 히드록시, 카르복시, 카르바모일, N,N'-디메틸카르바모일, 카르바모일옥시, 산소, 황, 질소원자를적어도한 개이상포함하고있는티오펜, 티아졸, 티아디아졸, 아미노티아졸, 이소티아졸, 이소옥사졸, 옥사졸, 옥사디아졸, 테트라졸, 피리딘의불포화 5환또는 6환헤테로고리치환체, 알킬, 할로겐, 알콕시, 시아노또는페녹시가치환된벤젠고리치환체, 약제학적으로허용되는염의메탄설폰산염, 퓨마렌산염, 브롬산염, 시트릭산염, 말레인산염, 인산염, 황산염, 나트륨염, 염산염또는염이아닌아민을포함한다.

公开(公告)号：KR1020000074955A

公开(公告)日：2000-12-15

申请号：KR1019990019242

申请日：1999-05-27

Applicant: 한국과학기술연구원

Inventor： 고훈영 ,  장문호 ,  조영서 ,  최경일 ,  배애님 ,  김혜연 ,  주현진

IPC: C07D413/14

Abstract: PURPOSE: Provided is an isooxazolyl carbonyl oxazolidinone derivative represented by the formula (I) which has an excellent antibacterial activity on gram-positive strain. Also, a preparation method of the compound is provided. CONSTITUTION: An isooxazolyl carbonyl oxazolidinone derivative represented by the formula (I) is prepared by acylation of oxazolidinone derivative of general formula (II) and carboxylic acid derivative of general formula (III) in the presence of a base and a solvent. R in the formula (II) and (III) is hydrogen, alkyl, halogen such as bromine or chlorine, cyano, alkoxy, hydroxy, carboxy, carbamoyl, N,N'-dimethylcarbamoyl, carbamoyloxy, oxygen, sulfur, thiopene having more than one nitrogen atom, thiazole, thiadiazole, aminothiazole, isothiazole, isooxazole, oxazole, oxadiazole, tetrazole, 5 or 6-membered unsaturated heterocycle substituent of pyridine, alkyl, halogen, alkoxy, benzene ring substituted with cyano or phenoxy group, pharmaceutically acceptable methanesulfonate, fumarate, bromate, citrate, maleate, phosphate, sulfate, sodium salt, hydrochlorate or amine not being salt.

Abstract translation: 目的：提供式（I）表示的异恶唑羰基恶唑烷酮衍生物，对革兰氏阳性菌株具有优异的抗菌活性。 此外，提供了该化合物的制备方法。 构成：由式（I）表示的异恶唑基羰基恶唑烷酮衍生物通过在碱和溶剂的存在下酰化通式（II）的恶唑烷酮衍生物和通式（III）的羧酸衍生物来制备。 式（II）和（III）中的R是氢，烷基，卤素如溴或氯，氰基，烷氧基，羟基，羧基，氨基甲酰基，N，N'-二甲基氨基甲酰基，氨基甲酰氧基，氧，硫， 一个氮原子，噻唑，噻二唑，氨基噻唑，异噻唑，异恶唑，恶唑，恶二唑，四唑，吡啶，烷基，卤素，烷氧基，被氰基或苯氧基取代的苯环的5或6元不饱和杂环取代基，药学上可接受的甲磺酸酯， 富马酸盐，溴酸盐，柠檬酸盐，马来酸盐，磷酸盐，硫酸盐，钠盐，盐酸盐或胺不是盐。