CAJ | 학술논문

目的研究头孢匹胺的合成工艺.方法 (R)2-(6-甲基-4-羟基吡啶-3-羰基)-氨基]-2-(4-羟基苯基)乙酸乙酯(NPA-Et)经水解、成盐得到(R)2-(6-甲基-4-羟基吡啶-3-羰基)-氨基]-2-(4-羟基苯基)乙酸钠(NPA-Na).NPA-Na与7-TMCA,即:(6R,7R)3-(1-甲基-1H-四唑-5-硫代甲基)-8-氧代-5-硫杂-1-氮杂双环[4.2.0]辛-2-烯-2-羧酸)缩合得头孢匹胺粗品,再成三乙胺盐,转酸,得到头孢匹胺成品.结果第一步收率84.6%,第二步收率69.3%.结论本工艺易操作,三废少,收率较高,为中试生产提供了依据.
목적 연구두포필알적합성공예.방법 (R)2-(6-갑기-4-간기필정-3-탄기)-안기]-2-(4-간기분기)을산을지(NPA-Et)경수해、성염득도(R)2-(6-갑기-4-간기필정-3-탄기)-안기]-2-(4-간기분기)을산납(NPA-Na).NPA-Na여7-TMCA,즉:(6R,7R)3-(1-갑기-1H-사서-5-류대갑기)-8-양대-5-류잡-1-담잡쌍배[4.2.0]신-2-희-2-최산)축합득두포필알조품,재성삼을알염,전산,득도두포필알성품.결과 제일보수솔84.6%,제이보수솔69.3%.결론 본공예역조작,삼폐소,수솔교고,위중시생산제공료의거.
Objective The process for synthesis of cefpiramide was studied.Methods(R)-2-[[(4-hydroxy-6-methyl-3-pyridinyl)carbonyl]amino]-2-(4-hydroxyphenyl)acetic acid ethyl ester(NPA-Et)was hydrolysized and then consendated with sodium salt to give(R)-2-[[(4-hydroxy-6-methyl-3-pyridinyl)carbonyl]amino]-2-(4-hydroxyphenyl)acetic acid sodium salt(NPA-Na).By preparing from NPA-Na and(6R,7R)-7-[[(2R)-[[(4-hydroxy-6-methyl-3-pyridinyl)carbonyl]amino](4-hydroxyphenyl)acetyl]amino]-3-[[(1-methyl-1H-tetrazol-5-yl)thio]methyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid(7-TMCA),the crude cefpiramide was getten,followed by formation of its triethylamine salt and then the salt was converted to the pure cefpiramide.Results The yield in the first step was 84.6% and it was 69.3% in the second step.Conclusion This process was prone to operate in high yield and the less three wastes while it provided a basis for pilot scale production.