7-苯乙酰氨基去乙酰氧基头孢G酸的制备

Preparation of 7-(Phenylacetamido)deacetoxycephalosporin Acid

以青霉素亚砜硅酯为原料经催化扩环制备头孢G酸。对 11种扩环催化剂进行了筛选 ,研制出了新型高效扩环催化剂MAB -Ⅱ ,使头孢G酸收率可达 93% (以质量计 ) ,w(C1 6 H1 6 N2 O4S) =( 93～ 96 ) %。其最佳工艺条件为 :n(C1 9H2 6 N2 O5 SSi)∶n(C8H1 0 NO) =1.0 0∶( 0 40～ 0 43) ;扩环温度 :10 5～ 10 8℃ ;扩环时间 :2 0～ 2 5h ;水解温度 :6 0℃ ;水解时间 :30～ 35min。以IR。

Phenylacetamido)deacetoxycephalosporin acid was synthesized from penicillin G Soxide trimethylsilyl ester and ringenlarging catalysts.Eleven sorts of catalysts were tested,among which one(MAB-Ⅱ) with high activity was found.The yield of the product could attain 93% and the content of the product was (93-96)%.The optimal molar ratio was n(C 19 H 26 N 2O 5SSi)∶n(C\-8H\-\{10\}NO)=1.00∶(040-043);the ringenlarging temperature was 105-108 ℃,the ringenlarging time was 20-25 h,the hydrolysis temperature was 60 ℃ and the hydrolysis time was 30-35 min.Moreover the structure of product was identified with IR and MS.