摘要
以苯乙酸和3甲氧基4苄氧基苯乙胺(1)为原料,通过1苯亚甲基2甲酰基6甲氧基7苄氧基3,4二氢异喹啉(4)的光环合得原小檗碱型碘化物(5),再经四氢硼钠还原、脱苄基合成了bharatamine(7),总收率达385%.放射配体受体结合试验表明该生物碱对多巴胺Ⅰ亚型受体有较强的亲和力.
From phenylacetic acid and 3methoxy4benzyloxy phenethylamine,bharatamine(7),a natural racemic protoberberine alkaloid,was synthesized via photocyclization of 1benzylidene2formyl6methoxy7benzyloxy3,4dihydroisoquinoline(4),followed by reduction with NaBH 4 and debenzylation with hydrochloric acid.The overall yield amounted to 385%.The receptor binding assays showed that the affinity of bharatamine to D 1 receptros was higher than that of stepholidine,and vice versa to D 2 receptors.
出处
《中国药物化学杂志》
CAS
CSCD
1998年第1期24-27,共4页
Chinese Journal of Medicinal Chemistry