天然糖分子增甜机理与构效关系的研究

以蔗糖、海藻糖、乳糖等天然糖分子为对象，使用选择性卤代试剂结合基团保护法对各游离羟基进行单一或不同组合的脱氧卤代衍生，分析其对衍生产物甜度大小、甜味特性优劣的影响规律，探索引起甜度变化的结构特点与结构优先性，建立糖分子的增甜机理与构效关系理论。选择１－２种具体的高甜度新型衍生物，作为新型强力甜味剂加以开发。

The sweetness of different sucrose halogenating derivatives were compared. Sweetness was enhanced through replacing C-4, C-1', C-6' hydroxyl groups of sucrose with hydrophobic groups, which was opposite to the result of replacement at C-6 hydroxyl group. A new kind of simple efficient synthetic method of sucralose with biosynthetic technology was put forward, with which quite pure sucrose-6-acetate, the key intermediate, was synthesized efficiently. As a result, the purity of sucralose reached 98% and the productivity reached 13.4% from sucrose. Also, sweetness changed after halogenating derivations on trehalose and lactose. The AH, B, X sweet triangle theory was developed by expanding the character of AH, B group and hydrophobic group X. The innemolecular hydrogen bond and the three-dimensional structure of sweetener molecular were also introduced into the theory for the same purpose. The solution properties of sweetener took a major effect on the sweetness. And the interaction between sweeteners and sweetness receptor protein had the same effect. A certain hydrophilic-lipophilic balance and effective interaction with sweetness receptor were needed for sweeteners. One monograph, 10 papers and 1 master dissertation were published.