采用黄连混合生物碱制备四丁氧基原小檗碱的工艺研究

Synthesis of tetra-n-butoxyprotoberberine from alkaloids in Coptids rhizoma

目的研究2,3,9,10-四丁氧基原小檗碱的合成工艺。方法以具有相似结构特征的黄连混合生物碱为起始原料,经脱甲氧基或亚甲二氧基、还原、丁基化、氧化4步反应,制备了目标产物。用1HNMR和ESI-MS鉴定目标产物。结果目标化合物经1HNMR和ESI-MS确证,总收率为14%。结论所用工艺适用于2,3,9,10-四丁氧基原小檗碱的批量生产。

OBJECTIVE To study the synthesis process of 2,3,9,10 -tetra- n -butoxyprotoberberine. METHODS It was synthesized from alkaloids in Coptids rhizoma with the similar structure of isoquinoline by a four - step reaction of alkaloids preparation ： demethylation or demethylene - dioxy, hydrogenation, butylation and oxidation. RESULTS The structure eftarget compound was confirmed by ^1 HNMR and ESI - MS, and the total yield was 14%. CONCLUSION This process is suitable for the batch production of 2,3,9,10 - tetra - n - butoxyprotoberberine.