头孢三嗪反式异构体合成研究

以头孢主环(6R,7R)-7-氨基-8-氧代-3-(1,2,5,6-四氢-2-甲基-5,6-二氧代-1,2,4-三嗪-3-基)硫代]甲基]-5-硫代-1-氮杂双环4.2.0]辛-2-烯-2-羧酸(7-ACT)为起始原料,与反式活性酯侧链(E)-2-(2-氨基-4-噻唑基)-2-甲氧亚胺-乙酸-2-苯并噻唑硫酯(E-AE)反应作用生成(6R,7R)-7-2-(2-氨基-4-噻唑基)-(E)-2-(甲氧亚胺)乙酰氨基]-8-氧代-3-(1,2,5,6-四氢-2-甲基-5,6-二氧代-1,2,4-三嗪-3-基)硫代〗甲基]-5-硫代-1-氮杂双环4.2.0]辛-2-烯-2-羧酸,然后在丙酮溶液中与异辛酸钠成盐而制得反式头孢三嗪钠。该产品具有良好的稳定性与高纯度,可作为对照品使用。

Improvement of the Synthetic Method of E-ceftriaxone

As the starting material （6R,7R） - 7 - amino - 8 - oxo - 3 - （ 1,2,5,6 - tetrahydro - 2 - methyl - 5,6 - dioxo - 1,2,4 - triazin - 3 - yl） thio ] methyl ] - 5 - Thia - 1 - azabicyclo 4.2.0 ]oct - 2 - ene - 2 - carboxylic acid （ 7 - ACT） ,the objective compounds E -ceftriaxone was condensed with the side chain compound （E） -benzo d] thiazol- 2 - yl -2 - （2 -aminothiazol- 4 -yl） -2 - （methoxyimino）ethanethioate on C7 -position via the active ester method. Then the condensed product E - ceftriaxone might be converted to its sodium salt with sodium isooctoate in the acetone solution. The product with the good stability and high purity was used to reference substance.