全基团保护法制备三氯蔗糖的研究

全基团保护法包括蔗糖 8个羟基团的完全保护、蔗糖 3个伯羟基的去保护作用、4 C位乙酰基向 6 C的迁移、对特定游离羟基团的氯化与脱除剩余保护基团等 5个步骤。其中 ,若采用碱性乙酰基迁移法 ,则乙酰基迁移与氯化反应 2步可合并为 1步。通过大量的试验 ,确定了具体的制备路线与各反应步骤之间的适宜组合方案 ,优化各种工艺参数 ,使三氯蔗糖终产品的得率达到 2 8 1 %。

Studies on the Hologroup Protected Synthesis of Sucralose

The hologroup protected synthesis method contained free octohydroxy groups protection of sucrose, deshielding of three primary protected hydroxy groups, acetyl migration from 4 C to 6 C, chlorination of particular desiginated free hydroxy groups and deshielding of other protected hydroxy groups The acetyl migration step , if with base environment, could be done together with the chlorination step The concrete synthesis routine and the appropriate combination of every reaction step were determined after many experiments, and various reactive parameters were optimized As a result, the productivity of sucralose reached 28.1% from sucrose.