三嗪青霉素是对绿脓肝菌有优异抗苗活性的广谱半合成青霉素。本文采用水合氧代丙二酸酯代替氧代丙二酸酯,并将其与氨基硫脲缩合,再经环合水解和氧化制成三嗪酸的四步反应改进为“一勺烩”的连续操作法,提高收率27.3%。三嗪酸与羟氨苄青霉素的缩合反应用价廉的氯甲酸乙酯代替氯甲酸异丁酯,提高了收率。又采用三嗪酸的琥珀酰亚胺活性酯对羟氨苄青霉素进行的酰化反应也获成功。 Triazine penicillin is a broad-spectrum semi-synthetic penicillin that has excellent anti-tumor activity against P. pyogenes. In this paper, hydrated oxo malonate was used instead of oxo-malonate, and then condensed with thiosemicarbazone. The four-step reaction of triazine acid by cyclization and oxidation was improved to “one scoop” Continuous operation, improve the yield of 27.3%. Triazine acid and amoxicillin condensation reaction with inexpensive ethyl chloroformate instead of isobutyl chloroformate to improve the yield. The acylation of amoxicillin by the succinimide active ester of triazine acid was also successful.