(1S,4S)-2-甲基-2,5-二氮杂二环[2.2.1]庚烷的合成

Synthesis of -2-Methyl-2,5-DiazabicycloHeptane

以N -位磺酰化的反 - 4 -羟基 -L -脯氨酸为原料 ,以硼氢化钾与氯化锌还原羧基 ,以三乙胺和丙酮代替吡啶进行羟基磺酰化和羟基氯代反应 ,“一锅煮”进行取代环合和去N -磺酰化合成 (1S ,4S) - 2 -甲基 - 2 ,5 -二氮杂二环 [2 .2 .1]庚烷 ,总收率达 5 3%。该法操作简便 ,收率高 ,更有利于工业化生产。

The N-tosylated trans-4-hydroxyl-L-proline is reduced with potassium borohydride and zinc chloride,tossylated and chlporinated with tosyl chloride in acetone and triethylamine,cyclization and cleavage might be finished in a 'one pot' processing . The total yield is 53%.The result shows that, the new synthetic method is simple in process, high in yield and feasible for industrial production.