氨曲南的合成

Synthesis of aztreonam

目的:以L-苏氨酸为起始原料,经N-Boc保护合成氨曲南。方法:以L-苏氨酸为原料,经酯化、氨解、氨基保护、保护羟基、磺化、环合、脱保护7步反应,制得氨曲南主环,并最终合成氨曲南。结果和结论:目标化合物经核磁共振氢谱确证其化学结构,收率60.4%(以氨曲南主环计)。该法工艺简单,反应效率提高。

Objective： To synthesize aztreonam starting from L-threonine via N-Boc protection. Methods： Started from L-threonine, the main-ring of aztreonam was prepared via esterification, aminolysis, and subsequent protection of amino group and hydroxyl group, sulfonation, cyclization, and deprotection. Results and conclusion ： The structure of aztreonam was verified by ^1H NMR. The overall yield was 60.4% （the main-ring of aztreonam）. This method is simple and has higher efficiency.