Extraction Of Lappaconitine, Preparation Of Lappaconitine's Ramification And Their Crystal Structures

Aconitum sinomontanum Nakai is own in China. The root is poisonous and officinal, and the efficacy is detumescent, acesodyne and can dredge blood, dispel chill. Lappaconitine is one of the main ingredients which extracted from the root of Aconitum sinomontanum Nakai. The main efficacy of lappaconitine is acesodyne. This paper found an optimal way to extract lappaconitine on the foundation of predecessors, and lappaconitine was charactered by FT-IR, MS, ¹H NMR, ¹³C NMR and element analysis The stereo configuration was made certain by X-ray single crystal experiment. The phenomena that lappaconitine hydrobromide was obtained but double quarter ammonium salt was not obtained by the reaction of lappaconitine and dibromine hydrocarbon was found firstly. In the salt of lappaconitine, the experiment prepared lappaconitine citrate, and lappaconitine tartrate. The paper found that unitary salt can be obtained, but multi-salt can not be obtained. The salts were charactered by FT-IR, ¹³C NMR and element analysis. The thesis consists of four parts as follows.Part I ReviewThe chapter summarizes the research development on the ways and means of extracting alkaloid, the main ingredients and officinal merits of Aconitum, the toxicity and the relation between the structure and the activity of Aconitum and the development of lappaconitine's reconstruction.Part II Extraction of lappaconitineOn the foundation of predecessors, this paper summarizes rules and finds an optimal way to extract lappaconitine, and make certain the stereo configuration. The structures of lappaconitine was characterized by IR, elemental analysis, ¹H NMR, ¹³C NMR and MS. The stereo configuration was made certain by X-ray single crystal experiment.Part III Preparation of lappaconitine's ramificationSection 1 Doubling lappaconitine molecules The phenomena that lappaconitine hydrobromide was obtained but double quarter ammonium salt was not obtained by the reaction of lappaconitine and dibromine hydrocarbon (Br-(CH₂)_n-Br, n=4, 6, 12) was found firstly. The reaction mechanism need more research. Lappaconitine hydrobromide was charactered by FT-IR, MS, ¹H NMR, ¹³C NMR and element analysis The absolute configuration was made certain by X-ray single crystal experiment. The chirality of C atoms was given.Section 2 Preparation of lappaconitine citrate and lappaconitine tartrateIn the salt of lappaconitine, the experiment prepared lappaconitine citrate, and lappaconitine tartrate. The paper found that unitary salt can be obtained, but multi-salt can not be obtained. The salts were charactered by FT-IR, ¹³C NMR and element analysis.Part IV The X-ray single crystal experiment of cinchonineThe single crystal was prepared, and the stereo configuration was confirmed by X-ray single crystal experiment.