(2R,3S)-3-苄氧羰酰胺基-4-甲基-2-氧代-1-氮杂环丁烷基磺酸钠的合成工艺改进

Improvement in the Synthesis of ( 2R,3S)-3-carbobenzyloxy amino-2-methyl-4-oxo-1-azetidinesulfonic Sodium

(2R,3S)-3-苄氧羰酰胺基-4-甲基-2-氧代-1-氮杂环丁烷基磺酸钠是合成氨曲南主环的重要中间体,我们以DMF与三氧化硫络合物取代强腐蚀性的氯磺酸进行磺化-环合反应,在DMAP与2-甲基吡啶复合催化剂的作用下产品收率较原工艺提高了约5%,降低了生产成本。

（2R, 3S） -3 - carbobenzyloxy - amino -2 - methyl -4 - oxo - 1 - azetidinesulfonic sodium is an important intermediate for synthesis of Aztreonam, we used DMF and sulfur trioxide complex to replace the chlorosulfonic acid which is highly corrosive for sulfonated - cyclization reaction, achieving good result, the yield of sulfonated -cyclization reaction was increased by about 5% compared with the original process and the cost of the production was reduced.