利奈唑胺的合成

Synthesis of Linezolid

对利奈唑胺合成工艺进行优化。以吗啉和3,4-二氟硝基苯为原料,经取代、还原反应得到中间体5;(R)-环氧氯丙烷7、邻苯二甲酰亚胺钾盐6发生取代反应合成中间体9;最后中间体5和9经取代、环化、水解合成目标产物利奈唑胺,总收率36.5%(以3,4-二氟硝基苯计)。

Linezolid was synthesized.The key intermediate 5 was synthesized from morpholine and 3,4-difluoronitrobenzene by substitution and reduction reactions.(R)-Epichlorohydrin 7 reacted with potassium phthalimide 6 by substitution to get intermediate 9.Finally,intermediate 5 reacted with intermediate 9 via substitution,cyclization and hydrolysis to afford the target compound linezolid with an overall yield of about 36.5%.