【摘要】 以7-甲氧基-2-萘满酮为原料合成了2-氨基-7-羟基四氢萘水合物。以苄胺与7-甲氧基-2-萘满酮反应,然后以硼氢化钠还原、盐酸酸化得到苄基保护的胺的盐酸盐,再以Pd/C催化氢解得到2-氨基-7-甲氧基四氢萘盐酸盐。将盐以碱处理得到2-氨基-7-甲氧基四氢萘,于无水乙醇中与扁桃酸反应分离手性异构体。分开的异构体先以NaOH中和,然后分别在48%的氢溴酸存在下水解得到2-氨基-7-羟基四氢萘的溴酸盐,再分别以氨水中和后得到2-氨基-7-羟基四氢萘两手性异构体的水合物。两异构体总收率均达到30%以上。更多还原

【Abstract】 2-Amino-7-hydroxytetralin monohydrate was synthesized from 7-methoxy-2-tetralone.7-Methoxy-2-tetralone reacted with benzylamine,then sodium borohydride was added for reduction and HCl was introduced for acidification to obtain hydrochloride of the benzyl-protecting amine.Hydrogenation of the hydrochloride was carried out with the existence of 5% Pd/C,and the hydrochloride of 2-amino-7-methoxytetralin was obtained.The salt was treated with alkali to obtain 2-amino-7-methoxytetralin,and the chiral mixture of 2-amino-7-methoxytetralin was separated by reacting with mandelic acid in absolute alcohol.The separated salt of the isomer with mandelic acid was neutralized with solution of NaOH,then hydrolyzed separately in solution of 48% hydrobromic acid,and the 2-amino-7-hydroxytetralin monohydrate was obtained separately after neutralizing with ammonia.The yields of both of the two isomers were up to 30%.更多还原