Lappaconitine derivatives and preparation method and application thereof

The invention relates to lappaconitine derivatives and a preparation method and application thereof. The lappaconitine derivatives are enantiomers, diastereoisomers, racemates, mixtures of the enantiomers, the diastereoisomers and the racemates, and pharmaceutically acceptable inorganic or organic salts, crystal forms and solvates of the enantiomers. The novel lappaconitine derivative is obtainedby adopting six preparation methods, the structure of diterpene alkaloid is enriched, the anti-arrhythmia and analgesic activity is superior to that of lappaconitine, and the toxicity is lower than that of lappaconitine, so that the synthesized lappaconitine derivative is applied to preparation of medicines for treating cardiovascular and cerebrovascular diseases and pains. 本发明涉及一种高乌甲素衍生物及其制备方法和用途，该衍生物为对映异构体、非对映异构体、外消旋体及其混合物以及其药学上可接受的无机或有机盐、晶型及溶剂合物，采用包含六种的制备方法得到的新型高乌甲素衍生物，丰富了二萜生物碱的结构，对抗心律失常和镇痛活性优于高乌甲素，且毒性小于高乌甲素，因此，合成的高乌甲素衍生物在制备治疗心脑血管和疼痛中的药物用途。