反应详情

A solution of 2-(2-tritylaminothiazol-4-yl)-(Z)-2-trityloxyiminoacetic acid (4.7 g, 7 mmol) (cf. Tetrahedron 1978, 34, 2233), 1-hydroxybenzotriazole (1.04 g, 7.7 mmol) and N,N'-dicyclohexylcarbodiimide (1.51 g, 7.35 mmol) in dimethylacetamide (27 ml) was allowed to react at room temperature for an hour. To the solution was added a solution of 7β-amino-3-[(1-amino-1H-tetrazol-4-yl)thiomethyl]-3-cephem-4-carboxylic acid (2.54 g, 7.7 mmol) and triethylamine (1.56 g, 15.4 mmol) in dimethylacetamide (20 ml) and water (0.5 ml) and the mixture was allowed to react at 5° C. for 1.5 hours. Then the mixture was treated in a manner similar to that described in Example 6, (c) to give pale yellow powder of 7β-[2-(2-tritylaminothiazol-4-yl)-(Z)-2-trityloxyiminoacetamido]-3-[(1-amino-1H-tetrazol-5-yl)thiomethyl]-3-cephem-4-carboxylic acid (2.86 g, 41.6%).

1. customto react at room temperature for an hour
2. customto react at 5° C. for 1.5 hours
3. additionThen the mixture was treated in a manner similar to