Xinjiang (?) Of The Active Ingredient And Its Analogues Research

Coniselin is a new natural compound isolated from the alcoholic extract of Coniselium vagination Thell. To provide sufficient sample for investigating its pharmacological activities, the total synthesis of this compound was carried out. The target molecule was prepared through a reaction sequence of nine steps in an overall yield of 16.3% using 3-Methoxy-4,5-dihydroxy-methy benzoate as starting material. The structure of synthetic coniselin was characterized by 1R, MS, ¹H-NMR, ¹³C-NMR data comparing with the natural compound. In order to research the relationship between the structure and activity, six kinds of its analogues were prepared.This paper provided a facile synthesis for preparing coniferyl alcohoi, which was carrried out by condensation of vanillin with monoethyl malonate, then by selective reduction. The operation was more simple and the yield was higher than those of reported methods ; In the presence of polyphosphoric acid (PPA), the monoamides of succinic and glutaric acids are readily cyclized, forming the corresponding succinimides and glutarimides. This synthetic method was not reported before.In addition, the acetyl cimicifugamide(a new natural compound isolated from Cimicifuge dahurica) was synthesized by four steps, the total synthesis of terrstriamide(isolated from Tribulus terrestris) and hypodematine (isolated from Hypodematium sinense Iwatsuki) were also studied.Pharmacological tests showed that nine compounds revealed some antitumour activities.87 compound and intermediates were synthesized, among them 51 compounds were new, further antitumour activities and heptoprotective activities are to be tested.