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本文包括以下步骤:在非质子性溶剂的存在下,一定的温度范围内,7-氨基头孢菌酸经硅烷化保护、碘取代、形成磷翁盐7-三甲基硅基氨基-3-三苯基磷亚甲基-4-头孢烷酸三甲基硅基酯后进行维蒂希反应、脱保护、结晶析出7-氨基-3-(Z-丙-1烯基)-4-头孢烷酸,以非亲和性碱为助溶剂,使其完全溶解后,与侧链对羟基苯酐氨酸酯类缩合,可得到7-【2-氨基-2-(对羟基-苯基)乙酰氨基】-8-氧代-3-丙烯基-5-硫杂-1-氮杂双环-2-烯-2-羧酸。
The present invention includes the following steps: 7-aminocephalosporanic acid is protected by silylation and substituted with iodine in the presence of an aprotic solvent at a certain temperature range to form a phosphonium salt 7-trimethylsilylamino-3-tris Phenyl Phosphoranylidene-4-cephemic acid trimethylsilyl ester, followed by Wittig reaction to deprotect and crystallize 7-amino-3- (Z-prop-1-enyl) Acid, with a non-compatible base as a cosolvent to completely dissolve it and condensation with a side-chain p-hydroxybenzoic acid ester to give 7- [2-amino-2- (p- hydroxy-phenyl) acetamido ] -8-oxo-3-propenyl-5-thia-1-azabicyclo-2-ene-2-carboxylic acid.