Study On Synthesis Of Novel Antidepressant Drug-Macholobemide And Antiamtha Drug-Seratrodast

Moclobemide, 4-chloro-N-[2-(4-morpholinyl)ethyl]benzamide, is one typical drug of the new kind of reversible monoamine oxidase inhibitor. It is applied in treating depressant effectively.Synthesis of Moclobemide was studied in the part one of dissertation. Based on the analysis and evaluation of bibliographer, the application of Moclobemide and its intermediates were reviewed. The processes for synthesis of moclobemide and its intermediates were evaluated.The Moclobemide was synthesized by condensation of morpholine with 4-chloro- N- (2-bromo- ethyl)benzamide which is prepared from the Schotten-Baumann reaction of 2-bromo-ethanamine hydrobromid and chloro- benzoyl chloride. The affect of the temperature of reactions and the ratio of the raw materials on the yield of the product were studied. The novel process was evaluated and the optimum process parameters were selected by experiments. The total yield of product is about 58.0%. The structure of the product and its intermediates were confirmed on spectral analysis.Seratrodast, 7-(3,5,6-trimethyl-l,4-benzoquinon-2-yl)-7-phenyl-hep-tanoic acid, is one typical drug of the new kind of antiasthma.Synthesis of Seratrodast was studied in part two of dissertation. Based on the analysis and evaluated of bibliographer, the applications of and its intermediate were reviewed. The processes for synthesis of Seratrodast were summarized.Starting from heptadioic acid, the main intermediate 7-hydroxy-7-phenylheptanoic acid was synthesized via esterfication, transesterfi-cation, acyl halidation, Friedel-Crafts reaction, reduction, hydrolyzation and Seratrodast was prepared from condensation reaction of 7-hydroxy-7-phenylheptanoic acid and trimethylhydroquinon. The novel process was evaluated and the optimum process parameters were selected. The total yield of Seratrodast is 11.7%.