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目的制备具有多种生物活性的菲并吲哚里西定类生物碱的关键中间体2-(3,6,7-三甲氧基菲-9-基-甲基)-2,5-二氢吡咯。方法以2,2,2-三氯-N-[1-(3,6,7-三甲氧基菲-9-基-甲基)-丁-2-烯基]乙酰胺为起始原料,经水解、Boc保护、N-烯丙基化、关环复分解反应及脱保护基共5步反应得到目标化合物。结果与结论合成了2-(3,6,7-三甲氧基菲-9-基-甲基)-2,5-二氢吡咯,其结构经1H-NMR谱确证,总收率为45.3%。
OBJECTIVE To prepare 2- (3,6,7-trimethoxyphen-9-yl-methyl) -2,5-dihydropteridin as the key intermediate of phenanthroindolizidine alkaloids with various bioactivities Pyrrole. Method Starting from 2,2,2-trichloro-N- [1- (3,6,7-trimethoxyphen-9-yl- methyl) -but-2-enyl] acetamide, After hydrolysis, Boc protection, N-allylation, ring-closure metathesis reaction and deprotection, a total of 5 steps to obtain the target compound. RESULTS AND CONCLUSION 2- (3,6,7-Trimethoxyphenanthrene-9-yl-methyl) -2,5-dihydropyrrole was synthesized and its structure was confirmed by 1H-NMR spectroscopy. The overall yield was 45.3% .