The Journal of Antibiotics
Online ISSN : 1881-1469
Print ISSN : 0021-8820
ISSN-L : 0021-8820
SYNTHESIS AND STRUCTURE-ACTIVITY RELATIONSHIPS OF 7β-[2-(2-AMINOTHIAZOL-4-YL)ACETAMIDO]CEPHALOSPORIN DERIVATIVES
IV. SYNTHESIS OF 2-(2-AMINOTHIAZOL-4-YL)-2-METHOXYIMINOACETIC ACID DERIVATIVES AND RELATED COMPOUNDS
MICHIHIKO OCHIAIAKIRA MORIMOTOYOSHIHIRO MATSUSHITATAIITI OKADA
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1981 Volume 34 Issue 2 Pages 160-170

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Abstract

In an effort to improve the antibacterial activity of 7β-[2-(2-aminothiazol-4-yl)acetamido]-cephalosporins by introducing a methoxyimino group into the 7-acyl side chain, geometrically isomeric 2-(2-aminothiazol-4-yl)-2-methoxyiminoacetic acids and their derivatives were selectively synthesized. Structurally related acid derivatives were also synthesized. A facile and practical synthesis of an important starting material, 2-(2-chloroacetamidothiazol-4-yl)-(Z)-2-methoxyiminoacetic acid, for the preparation of SCE-1365 which is now under extensive clinical trial was achieved.

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© Japan Antibiotics Research Association
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