以间甲氧基苯乙胺和氯甲酸乙酯为原料,通过亲核取代、关环、四氢铝锂还原得到1,2,3,4-四氢异喹啉衍生物.其中关键步骤环化反应实现了使用多聚磷酸(PPA)简便有效地进行了关环,合成了一系列异喹啉酮类衍生物.
1,2,3,4-Tetrahydroisoquinoline derivatives were synthesized from 2-(3-methoxyphenyl)ethy-lamine and ethyl chloroformate via the process of nucleophilic substitution,cyclization reaction and lithium aluminium hydride(LAH) reduction.The key step,cyclization reaction,was accomplished by using polyphoshponic acid(PPA) as a catalyst conveniently and effectively without any another catalyst for the first time.Moreover,a series of isoquinolone derivatives were synthesized.