青霉素G亚砜二苯甲酯的合成研究

Synthesis of Penicillin G Sulfoxide Diphenylcarbinol Ester

以青霉素G钾为原料制备青霉素G亚砜二苯甲酯。氧化反应优化条件为:n(过氧乙酸)∶n(青霉素G钾)=1.2∶1.0,氧化温度0～5℃,反应时间2h,青霉素G亚砜酸收率为97.3%;酯化反应优化条件为:二氯甲烷的用量为17mL/g青霉素G亚砜,投料比n(二苯甲醇)∶n(青霉素G亚砜)=1.8∶1.0,反应温度为-15℃,反应时间为60min,酯化收率为79.5%,反应总收率为77.4%。此工艺成本低廉,操作安全简便,对工业化生产具有积极意义。

Penicillin G sulfoxide diphenylcarbinol ester was synthesized by penicillin G potassium salt. The yield of penicillin G sulfoxide was 97.3% under the conditions which the molar radio of acetic hydroperoxide to penicillin G potassium was 1.2：1.0, the oxidization temperature was 0-5℃, and the reaction time was 2 h; The optimal conditions of esterification was the amount of penicillin G sulfoxide and methylene chloride were 1 g and 17 mL, the molar radio of diphenylcarbinol to penicillin G sulfoxide was 1.8：1.0, the reaction temperature was -15℃, the reaction time was 60 min, the yield of penicilin G sulfoxide diphenylcarbinol ester was 79.5%, and the total yield was 77.4%. This technology was suitable to industrial production because of cheapness and safety.