1.study On The Synthesis Of Antipsychotic Drug Aripiprazole 2.studies On The Synthesis Of Isoquinoline Derivatives

Part 1.Study on the Synthesis of Antipsychotic Drug AripiprazoleSchizophrenia is one kind of mental illness.Positive symptoms include hallucinations,delusions,and disorganized thought.Negative symptoms include depression and withdrawing the society relationships.Schizophrenia has been bringing great pains to the patients.The development synthesis of antipsychotic drug and then the process of the preparation of the atypical antipsychotics aripiprazole (7-[4-[4-(2,3 -dichlorophenyl)- 1 -piperazinyl]butoxy]-3,4-dihydro-2(1H)-quinolinone) was reviewed in this paper.Firstly,diethanolamine reacted with hydrobromic acid to form N,N-dibromethylamine,and then reacted with 2,3-dichlorophenyl-amine to get 1-(2,3-dichlorophenyl)piperazine,m-Anisidine was used as the starting material,and reacted with 3-chloropropionylchloride to form 3-chloro-N-(3-methoxyphenyl)-propionamide, which was used to prepared 7-hydroxy-3,4-dihydro-2(1H)-quinolinone by Friedel-Crafts reaction in the presence of AlCl₃,and then treated with 1,4-dibromobutane to give 7-(4-bromobutoxy)-3,4-dihydro-2(1H)-quinolinone.Then the product reacted with 1-(2,3-dichlorophenyl)piperazine to get aripiprazole.The procedure is convenient to operate and the method is suitable for industrial manufacture.The structure of target compounds was confirmed by ¹H-NMR and MS and so on.Part 2.Studies on the Synthesis of Isoquinoline DerivativesThe isoquinolyl-alkaloids have been taking the important positions in the natural product chemistry.Systematically studying the chemical activity and biological activity of isoquinolyl-alkaloids is benefit to search the active lead compound and further develop new medicine.5-Bromoisoquinoline was synthesized as the key intermediate by using isoquinoline as start material.Several isoquinoline derivatives were synthesized from 5-bromoisoquinoline in this paper,including 5-bromo -8-nitroisoquinoline,8-aminoisoquinoline,8-bromoisoquinoline and so on.Some other isoquinoline derivatives,including 7-hydroxyisoquinoline,7-methoxy-isoqui-Noline, 7-bromoisoquinoline,7,8-dichloroisoquinoline,6,7-dimethoxy- isoquinoline, 6,7-dichloroisoquinoline,were synthesized through cycling reaction.Their possible chemical reaction mechanism was discussed.The expectation of isoquinoline derivatives drugs was also given.The structure of all target compounds was confirmed by MS and ¹H-NMR and so on.