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国产盐酸头孢甲肟的制备 被引量:7

The preparation process of domestic cefmenoxime hydrochloride
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摘要 以3-[[(1-甲基-1H-四唑-5-基)硫]甲基]-7-氨基-头孢烷酸盐酸盐(7-ATCA.HC l)为原料,在C7-NH2位置上用活性酯法与侧链化合物2-(2-氨基-4-噻唑基-2-(Z)-甲氧亚胺基乙酸缩合得到头孢甲肟,然后在水溶液中与盐酸成盐而制得盐酸头孢甲肟。以7-ATCA.HC l为基准,总合成收率在66%以上,产物为高纯度结晶性粉末。 This paper describes the preparation process of cefmenoxime hydrochloride [(CMX)_2·HCl]. 3-[(1-methyl-1H-tetrazol-5-yl-thio)-methyl]-7-amino-cephalosporanic acid hydrochloride (7-ATCA·HCl) as the starting material, was condensed with the side chain compound 2-(2-amino-4-thiazol)-2(z)methyloxy-imino acetic acid on C_7- position via the active ester method and then the condensed product cefmenoxime (CMX) might be converted to its hydrochloride [(CMX)_2·HCl]. The total yield of the process was more than 66% (based on 7-ATCA·HCl). The product was obtained as a crystalline powder in high purity.
出处 《中国抗生素杂志》 CAS CSCD 北大核心 2005年第7期396-398,共3页 Chinese Journal of Antibiotics
关键词 头孢甲肟 盐酸头孢甲肟 7-ATCA·HCl 氨噻肟乙酸 合成 Cefmenoxime Cefmenoxime hydrochloride 7-ATCA·HCl 2-(2-amino-4-thiazol)-2(z)methyloxy-imino acetic acid Synthesis process
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  • 1Cefmenoxime preparations [J]. Jpn J Antibiot, 1982, 35(11):2615
  • 2Ochiai M, Okada T, Aki O, et al. Thiazolylacetamido cephalosporin type compounds [P]. US 4098888, 1978-07-04
  • 3Heymes R, Lutz A. Alkyloximes of 7-amino-thiazolylacetamido-cephalosporanic acids [P]. US 4476122, 1984-10-09
  • 4Ochiai M, Morimoto A, Miyawaki T, et al. Synthesis and structure-activity relationships of 7 beta-[2-(2-aminothiazol-4-yl)acetamido]cephalosporin derivatives. Ⅴ. Synthesis and antibacterial activity of 7 beta-[2-(2-aminothiazol-4-yl)-2-methoxyiminoacetamido]-cephalosporin derivates and related compounds [J ]. J Antibiot (Tokyo), 1981,34(2):171
  • 5Ochiai M, Morimoto A, Miyawaki T. Synthesis and structure-activity relationships of 7 beta-[2-(2-aminothiazol-4-yl)acetamido]cephalosporin derivatives. Ⅵ. Alternative syntheses of 7 beta-[2-(2-aminothiazol-4-yl)-(Z)-2-methoxyiminoacetamido]cephalosporin derivatives [J].J Antibiot (Tokyo), 1981,34(2): 186

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