The Synthesis Of Tetrahydropalmatine

Tetrahydropalmatine,which is naturely existed in the root of Menispermaceae plants hua daughter cane,is a kind of the tetrahydroberberine analogous alkaloids and could be prepared from extraction,also chemosynthesis and biosynthesis.It is proved to have activities such as relieve pain and hypnosis used in the therapy of gastrohelcoma,duodenal ulcer pain,cramps,childbirth succedent houses shrink pain,Tension insomnia,spasmodic cough,auricular fibrillation, and also restrained the people leukemia cell line in combination with vincristine.As the increase of clinical dosage and the limitation of natural medicine,it has an important significant sense to develop a synthetic route of Tetrahydropalmatine which is safety,reasonable and economical.In order to achieve the synthetic process of Tetrahydropalmatine, retrosynthetic analysis is needed to found the intermediate of Tetrahydropalmatine and then synthesised. Tetrahydropalmatine was synthsized from 3,4-Dimethoxyphenethylamine and 2,3-Dimeth-oxybenzaldehyde via six steps,such as condensation,reduction of KBH4,acylation,Friedel-Crafts,Bischler-Napieralski reaction,reduction of NaBH4.The experiment result shows that the designed route of Tetrahydropalmatine is feasible,the structure of the intermediate and target compound were characterized by 1HNMR.but better improvement remain needed because the side reaction and low yield which lead to the lower overal yield during the preparation of some intermediates.