发明名称 3-(ISOTHIAZOLE)THIOMETHYL-DELTA3-CEPHEM-4-CARBOXYLATE DERIVATIVE AND ITS PRODUCTION
摘要 <p>NEW MATERIAL:A compound of formula I [R<1> is lower alkyl which may be substituted with carboxyl; R<2> is H, ester residue; R<3> is H, halogen, hydroxyl, lower alkyl, lower alkoxy amino] or its salt. EXAMPLE:7-(Z)-[alpha-( 2-aminothiazol-4-yl )-alpha-(methoxyimino)acetamide]-3-(isothia zole-3-yl)thiomethyl-DELTA<3>-cephem-4-carboxylic acid. USE:Antibacterial against gram-positive and -negative bacteria. It is good in intestinal absorption on oral administration. PREPARATION:The reaction between 7-substituted or unsubstituted amino-3-(isothiazole)thiomethyl-DELTA<3>-cephem-4-carboxylate derivative of formula II (R<4> is H, tri-lower alkylsilyl; R<5> is H, carboxyl-protecting group) and alpha-(2- substituted-4-thiazole)-alpha-substituted iminoacetic acid of formula III (R<6> is H, amino-protecting group; R<7> is lower alkyl) give the compound of formula I.</p>
申请公布号 JPS63267790(A) 申请公布日期 1988.11.04
申请号 JP19870101651 申请日期 1987.04.23
申请人 YAMANOUCHI PHARMACEUT CO LTD 发明人 MAEDA TETSUYA;HARA RYUICHIRO;NAGANO KENSHO
分类号 C07D513/04;A61K31/54;A61P31/04 主分类号 C07D513/04
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