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研究了以三氯化铁为催化剂选择性合成普罗布考单丁二酸酯的反应。考察了催化剂、反应溶剂、碱、酰化剂及配料比对反应的影响。实验结果表明金属盐对反应的收率和单酰化反应的选择性有显著的影响,当以三氯化铁为催化剂,丁二酸酐为酰化剂,叔丁醇钠为碱,四氢呋喃为溶剂,普罗布考、叔丁醇钠、丁二酸酐及三氯化铁的摩尔比为1∶4∶5∶0.17,反应温度为室温,反应时间为1h时,普罗布考单丁二酸酯的产率可达55%。
The reaction of selective synthesis of probucol monosuccinate with ferric chloride as catalyst was studied. The effects of catalyst, reaction solvent, base, acylating agent and ingredients ratio on the reaction were investigated. The experimental results show that the metal salt has a significant effect on the yield of the reaction and the selectivity of the monoacylation reaction. When using ferric chloride as catalyst, succinic anhydride as acylating agent, sodium tert-butoxide as base and tetrahydrofuran as solvent , Probucol, sodium tert-butoxide, succinic anhydride and ferric chloride molar ratio of 1: 4: 5: 0.17, the reaction temperature was room temperature, the reaction time was 1h, probucol monosuccinate Yield up to 55%.