头孢雷特中间体2-氨甲基苯乙酸的氨基保护

Protection of Amino Group in the 2-Aminomethylphenylacetic Acid,the Intermediate of Ceforanide

头孢雷特是临床中常用的第二代头孢类抗生素，其临床应用前景十分看好。2-氨甲基苯乙酸是生产头孢雷特的重要中间体，由于该化合物中同时存在氨基和羧基两个活性集团，因此，在生产中需要先将氨基进行保护，以便羧基进行下一步反应。

The amino-group of 2-aminomethylphenylacetic acid was protected by tert- butyloxycabonyl(BOC)group,the protection was conducted via condensation in the mixed solvent composed of dioxane,dichloromethane and water in the presence of NaOH or triethylamine.The optimal reaction conditions were determined and the optimum yield could be reached up to 88.1%.The structure of target product was confirmed by IR,HPLC and NMR.