以乳糖为原料设计合成了半乳凝素-3的潜在抑制剂—1-O′烯丙基-4-O-{3-脱氧-3-[4-苄胺羰基-1H-(1,2,3)三氮唑-1-基]-β-D-吡喃半乳糖基}-2-脱氧-2-乙酰氨基-β-D-吡喃葡萄糖。乳糖2-位的改造采用了叠氮-碘糖基化法,在乙酰氨基引入的同时立体选择性地构建了β-氨基乳糖苷;通过两次构型翻转在3′-位引入叠氮基,然后采用Click反应构建出三氮唑羧基,再与苄胺反应便得到目标物。对乳糖的上述改造旨在提高其对半乳凝素-3的亲和活性。 The potential inhibitor of galectin-3 was designed and synthesized using lactose as raw material. 1-O ’Allyl-4-O- {3-deoxy-3- [4-benzylaminocarbonyl-1H , 3) Triazol-1-yl] -β-D-galactopyranosyl} -2-deoxy-2-acetamido-β-D-glucopyranose. The modification of lactose 2-position adopts the azide-iodosylation method, which forms the β-amino lactosyl glycoside stereoselectively when the acetamido group is introduced; the azide group is introduced at the 3’-position by two configuration inversion , And then use the Click reaction to create a triazole carboxyl, and then react with benzylamine to get the target. The above modification of lactose aims to increase its affinity for galectin-3.