反应详情

A solution of 7β-[2-(2-aminothiazol-4-yl)-2-(Z)-(trityloxyimino)acetamido]-3-[(pyrazin-2-yl)methylthio]-3-cephem-4-carboxylic acid (1.5 g, 2.04 m mol) in 90% formic acid aqueous solution was stirred at room temperature for 2 hours. Insoluble material in the reaction mixture was filtered off. The filtrate was adjusted to pH 3 and washed with ethyl acetate. The aqueous solution was chromatographed on HP-20 and eluted with 5-14% isopropanol aqueous solution. The eluent was lyophilized to give crude product (275 mg). The crude product was purified with preparative HPLC to give 7β-[2-(2-aminothiazol-4-yl)-2-(Z)-(hydroxyimino)acetamido]-3-[(pyrazin-2-yl)methylthio]-3-cephem-4-carboxylic acid (131 mg, 0.265 m mol).

1. filtrationInsoluble material in the reaction mixture was filtered off
2. washwashed with ethyl acetate
3. customThe aqueous solution was chromatographed on HP-20
4. washeluted with 5-14% isopropanol aqueous solution
5. customto give crude product (275 mg)
6. customThe crude product was purified with preparative HPLC