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5-溴-2-氟苯酚(1)是抗抑郁药木防己苦毒宁(picrotoxinin)的中间体,也可用于合成其他化合物进行新药研究。1的合成路线主要有以下4种:①以对氟溴苯为原料,与丁基锂反应活化氟原子邻位后,与三丙基硼酸盐或三甲基硼酸盐反应得到5-溴-2-氟硼酸,再经氧化、水解得到1。此路线在丁基锂活化时需在2,2,6,6-四甲基哌啶的THF溶液中反应,无水无氧且后处理操作繁琐。②文献用“一锅煮”
5-Bromo-2-fluorophenol (1) is an intermediate of the antidepressant picrotoxin and can also be used to synthesize other compounds for new drug research. 1 synthesis route mainly has the following four kinds: (1) to bromine bromobenzene as raw material, and butyllithium reaction of fluorine atoms ortho, with tripropyl borate or trimethyl borate to give 5-bromo 2 - fluoroboric acid, and then by oxidation, hydrolysis 1. This route requires the reaction of butyllithium in THF solution of 2,2,6,6-tetramethylpiperidine, anhydrous and oxygen-free and the post-treatment operation cumbersome. ② literature with “a pot”