青霉素亚砜酯的制备及精制

Preparation and Purification of Penicillin Sulfoxide Ester

青霉素亚砜酯是合成GCLE的重要中间体。以青霉素G为原料,甲醛作溶剂、过氧乙酸为氧化剂,经过酯化和氧化反应,得到青霉素亚砜酯粗品;以丙酮和水作为溶剂,经过丙酮加热、重结晶等制得青霉素亚砜酯精品。结果表明,目标产物含量达到99.5%以上,总收率为91.18%。该精制工艺过程简单,提高了产品质量,适于工业化生产。

Penicillin sulfoxide ester is an important intermediate of synthesis of GCLE.Firstly the crude peniciuin suifoxide ester was synthesized with toluene as solvent,acetic acid peroxide as oxidant by esterification and oxidation reaction.Secondly through dissolution of the crude product and recrystallization,the target product was obtained with penicillin G as raw material.The results showed that the product content was increased to more than 95%,the total yield reached 91.81%,this process was simple,could improve the product quality,be suitable for industrial production.