头孢唑肟丙匹酯的合成

Synthesis of Ceftizoxime Alapivoxil

(6R,7R)-7-氨基-8-氧代-5-硫-1-氮杂二环[4.2.0]辛-2-烯-2-羧酸与(Z)-2-[[[(S)-2-(叔丁氧羰基)氨基-1-氧代丙基]氨基]-4-噻唑基]-2-甲氧亚氨基乙酸(2-巯基苯并噻唑)酯反应制得(6R,7R)-7-[[[2(S)-[(N-叔丁氧羰基-2-氨基-1-氧代丙基)-氨基]-4-噻唑基][(Z)-甲氧基亚氨基]乙酰基]氨基-8-氧代-5-硫-1-氮杂二环[4.2.0]辛-2-烯-2-羧酸,与特戊酸碘甲酯成酯后,再脱保护、成盐制得头孢唑肟丙匹酯单盐酸盐,总收率为72%。

Ceftizoxime alapivoxil monohydrochloride was synthesized from （6R,7R）-7-amino-8-oxo-5-thia-1- azabicyclo [4.2.03 oct-2-ene-2-carboxylic acid and 2-mercaptobenzothiazolyl （Z） -2- E E E （S） -2- （t-butoxycarbonyl） amino- 1-oxopropyl] amine]thiazol-4-yl]-2-methoxyiminoacetate by condensation, esterification with iodomethyl pivalate, deprotection and then salt formation with an overall yield of 72 %.