Study On The Synthesis And The Technology Summary In Pilot Production Of Aripiprazole

Aripiprazole is a carbostyril derivatives. It is developed by Otswka corporation and Bristol-Myers Squibb corporation, used to treat schizophrenia and mania phase of bipolar disorder. And it was approved by FDA in November, 2002.An Industrial synthetic method of aripiprazole was described in this thesis through the modification and optimization of the reaction condition.Aripiprazole was prepared by several steps from m-aminoanisole, through acylation , Friedal-Crafts reaction, etherification, condensation and Purification. The total yield for Aripiprazole was 19% from m-aminoanisole. The structure of Aripiprazole was stated by IR, Elementary analysis, NMR and MS. And the polymorph of Anhydrous B was stated by IR, XRD and DSC.Based on the synthetic method, prepared the pilot process . According to the pilot process, calculated the material balance , designed the technological equipment flow chart and equipped the pilot equipment. At last, Completed the pilot production successfully.In this process, the reaction steps is more short than others , the reaction conditions is not strictly , the operation is easily to control and the waste water, gas and solid can easily to deal with. The process is suitable for industrial manufacture.