【摘要】 目的:改进磺苄西林钠的合成工艺。方法:以苯乙酸为原料,经磺化、手性拆分、酰氯化后,再与6-氨基青霉烷酸(6-APA)缩合、成盐制备磺苄西林钠。结果:对磺化反应和缩合反应进行了工艺改进。反应总收率为46%,产品结构经IR、1HNMR等数据确证。结论:本工艺操作过程简单,反应时间缩短,收率提高,适合工业化生产。更多还原

【Abstract】 Aim:To improve the synthesis process of sulbenicillin disodium.Methods:Sulbenicillin disodium was prepared by the condensation of the triethylamine salt of 6-aminopenicilanic acid(6-APA) and D(-)-sulfophenyllacetyl chloride.The latter was prepared from phenylacetic acid by sulphofication,followed by chiral resolution with L-lysine hydrochloride and further chlorination.Results:The processing condition of sulphofication and condensation was improved with the overall yield of 46%.The structure of the title compound was characterized by IR and 1H NMR.Conclusion:The synthesis process with shorten reaction time and increased yield was achieved and can be applicable in industry.更多还原