Synthesis And Acaricidal Activity Of N-Aryl-3,4-dihydroisoquinolines Bromides

Benzo[c]phenanthridine(QBAs),like chelerythrine, sanguinarine, is a member of isoquinoline alkaloid, which has distinct activities, such as antitumoral, antiviral, antimicrobial and insecticidal activities. However, the research of QBAs is limited due to the shortage of species and its natural content. It's a convenient way to acquire Benzo[c]phenanthridine or the derivatives with similar structure of good effects by organic synthesis and general bioliogical activities evaluation.Our reaserch focus on N-aryl-3, 4-dihydroisoquinolines on two follow aspects: Firstly, we describe the synthesis of 3, 4-dihydroisoquinolines through three steps with paraformaldehyde, 2-phenylethanol as substrates. N-aryl-3,4-dihydro- isoquinolines were synthesized and analyzed by 1H NMR, 13C NMR, ESI-MS, IR, UV. With N-phenyl-3,4-dihydroisoquinolines, 1-methoxy- N-phenyl-3,4-dihydro- isoquinoline was gotten. This method is high effective, universal and convenient to synthesize related compounds.Secondly, we conducted the acaricidal activity analysis. Psoroptes (P.communis cuniculi), isolated from rabbits, was used to evaluate the acaricidal activity of target molecules. Liner regression model was conducted to analyze the average mortality at different target molecules and different concentrations, and SPSS was adopted to analyze the significance of different mortality of compounds at 0.4 mg/mL. All compounds show acaricidal activity at different grade. Finally, 15 compounds were selected which have significant acaricidal activity comparing with Avermectins. And, it's potential to give more attention to these compounds on research and exploration.