2-苄基-6-对甲苯磺酰基-2,6-二氮杂螺[3,3]庚烷的合成

Synthesis of 2-Benzyl-6-tosyl-2,6-diazaspiro[3,3]heptane

以三溴新戊醇为原料,经与对甲苯磺酰胺环合、环醚开环、羟基活化、环合等4步反应以58%的收率合成了目标产物,相比已有合成方法,该合成路线以甲磺酰基(-OMs)离去基替代溴原子,提高了收率、简化了反应的操作和后处理,适合工业化生产。

The 2-benzyl-6-tosyl-2,6-diazaspiro[3,3]heptane was synthesized by the reaction of cyzlization with p-toluenesulfonamide,ring opening of ether,activation of hydroxyl group and cycalization from pentaerythritol tribromide as raw material with 58%total yield.By using the methylsulfonyl group（-OMs）instead of Br,the modified synthetic route is privileged with higher yield,more simple operation and especially suitable for industrial production.