1,3-二羰基化合物烯丙基化构建季碳中心的反应研究

Allylation of 1,3-dicarbonyl compounds to construct quaternary carbon centers

许多天然产物和药物活性分子往往因为季碳中心的存在而表现出更好的理化性质和生物活性.文章首先以氢化钠作碱,利用酮和酯反应得到了一系列的α-取代-1,3-二羰基化合物,收率50%～87%;然后进一步通过烯丙基化反应成功合成了具有3个官能团(2个羰基和1个烯基)的季碳砌块,产率为50%～93%.并对合成的α-取代-1,3-二羰基化合物和烯丙基化产物进行了1H NMR表征.

Many natural products and active pharmaceutical molecules with quaternary carbon center tend to show better physical and chemical properties and biological activity. Herein a series of α-substituted-1 ,3- dicar- bonyl compounds were synthesized from the reaction between ketone and ester with sodium hydride as base and then were allylated to construct quaternary synthetical building-block with muhifunctional groups in yield 75 % to 93%. All the products were characterized by 1H NMR.