The Synthesis Of Anticoccidial Drug Intermidate And Substituted 2-quinolines Aldehyde

As various medicine intermediate,p-trifluoromethylthiophenol is widely used in the medical chemistry,especially on the synthesis of anticoccidial drug toltrazuil.With the active trifluoromethyl in drug,it can not only improve the drugs'liposolubility,but also increase the stability.In this thesis,the synthesis of toltrazuil intermidate is optimized and we also studied the synthesis of 2-quinolines aldehyde.This thesis is consists of two parts.The first chapter presents an overview of the toltrazuil and its key intermidate.Some selectively trifluoromethylation on hydrosulfuryl was summarized.The synthesis of p-trifluoromethylthiophenol from p-hydroxythiophenol and trifluoromethyl bromide using sodium hyposulfite as initiator has been optimized.Hazardous substances as well as a lot of waste water were avoided in this new process,which is in line with the requirements of green chemistry.The second chapter was briefly described 2-quinolines aldehyde and introduced several methods to synthesize 2-quinolines aldehyde.A rapid and efficient one-pot Iron/O₂-promoted hydroformylation of 2-methylquinolines to produce 2-quinolines aldehyde under microwave irradiations has been achieved.Advantages of this method include the easy operation,short reaction time and good selectivity.