The Synthesis And Optimization Of Phosphodiesterase Inhibitor Rolipram And Series Of Drug Building Blocks

This dissertation is divided into two parts. In the first part, the Phosphodiesterase Type IV Inhibitor --Rolipram was studied, which have the structure of five number lactam . summarized the synthesis strategy and clinic pharmacodynamical of Rolipram , designed a concision route and finished it. This method is adapt to industrial produce.In part two, several normal building-block was researched and preparationed. We synthesized the kind of compound which included fluorin-substituted benzene. 2-(trifluoromethoxy)benzensulfonamide (pesticide intermediate),2,3,5,6-tetrafluoroterephthalic acid (medicament intermediate) and 7-chloro-1-cyclopropyl-6-fluoro-4-di hydroquinoline-3-carboxylic acid. The application of ring-closingrection we got the imidazole. An efficient method for rapid preparation of heterocyclic imidazole and heterocyclic pyrazole. The good yield was given.We also researched the industry product-condition of building-block. These strategy provide efficient methods to access building-block based on reaction mechanism that are of great interest in drug synthesize industry.