【摘要】 以L-丙氨酸为原料,经二碳酸二叔丁酯保护氨基、CDI缩合酰胺化反应、Mitsunobu反应、HCl去保护四步反应,以59.4%的总收率合成了(R)-1,3-二甲基哌嗪-2-酮,其结构经~1H NMR确认无误,并对分子内Mitsunobu反应条件进行了优化。与其它合成路线的研究结果相比较,该路线减少了副产物反应的发生,缩短了反应步骤,降低了分离难度,提高了收率和产品纯度,更适合规模化合成。更多还原

【Abstract】 Started from L-alanine,( R)-1,3-dimethylpiperazin-2-one was synthesized by four steps of reaction:protected by di-tert-butyl dicarbonate,condensed amidation reaction with CDI,Mitsunobu reaction and deprotected with HCl,at a total yield of 59. 4%. Structure of products was characterized by1 H NMR and the Mitsunobu reaction conditions were optimized. Compared with the results of other synthetic routes,the synthesis suppressed side reactions,shortened the reaction steps,reduced the difficulty of separation,improved yield and product purity,was suitable for large-scale synthesis.更多还原