A PROCESS FOR THE PREPARATION OF ANHYDROUS POLYMORPHIC FORM OF OLANZAPINE

摘要

Malononitrile is reacted with Propionaldehyde in presence of Sulphur Powder and Triethylamine in N,N-dimethlyformamide to give 5-Amino4- Cyano-2 -Methyl Thiophene. 2-fluoronitrobenzene is condensed with 5- Amino-4-Cyano-2-Methyl Thiophene in Isopropyl alcohol and Potassium Hydroxide powder give 4-cyano-2-methyl-1-(2-nitrophenyl amino) Thiophene. Reduction of 4-cyano-2-methyl-1-(2-nitrophenyl amino) Thiophene with Stannous Chloride and Hydrochloric acid in Isopropyl; Alcohol and followed by cyclization to get 4-Amino-2-Methyl-10H- Thieno [2,3,-b][1,5] Benzodiazepine Condensation of 4-amino-2-methyF10H-Thieno [2,3,-b][1,5] Benzodiazepine and N-methyl Piperazine in presence of Dimethyl Sulphoxide and Toluene gives Olanzapine Technical grade, in anhydrous form. Treatment of anhydrous technical Olanzapine with acetone followed by subsequent precipitation with an anti solvent gave anhydrous OLANZAPINE of Form-II.