Improvement of the synthetic method of anastrozole

Anastrozole was synthesized via six reaction steps of carbonylation,methylation chlorination,cyanidation,bromination and N-alkylation using 3,5-Dibromotoluene as the starting material.The factorssuch as different catalysts,the reaction time and reaction temperature had been investigated.Sodium hydride was used as the bind acid agent to avoid the produce of the isomer.The reaction conditions were described as follows PdCl2(PPh3)2 as catalysts and Et3N as alkali,the reaction was heated at 90 ℃ under 9.12×106 Pa.The total yield was 55.2%.The structure of final product was confirmed by 1HNMR and MS.Compared with the methods in pafent,this method was more simple to operate with low cost and high yield and was also more suitable for the large scale production.