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D-果糖经丙酮缩合后用硫酰氯氯磺酰化制得2,3:4,5-双-O-(1-甲基亚乙基)-β-D-吡喃果糖氯磺酸酯,再以碳酸铵进行氨解制得目标化合物托吡酯(1),总收率77%。按此方法制得1类似物1,2:5,6-双-O-(1-甲基亚乙基)-α-D-呋喃葡萄糖氨基磺酸酯(2)和1,2:3,4-双-O-(1-甲基亚乙基)-α-D-吡喃半乳糖氨基磺酸酯(3),总收率分别为45%和80%。
D-fructose is condensed with acetone and then chlorosulfonated with sulfuryl chloride to prepare 2,3: 4,5-bis-O- (1-methylethylidene) -β-D-fructopyranose chlorosulfonate, Ammonia was further hydrolyzed with ammonium carbonate to give the target compound topiramate (1) in a total yield of 77%. 1 analogues 1, 2: 5,6-bis-O- (1-methylethylidene) -alpha-D-glucopyranosulfamate (2) and 1,2: 3, 4-bis-O- (1-methylethylidene) -α-D-galactopyranosyl sulfamate (3) in 45% and 80% overall yield, respectively.