Wuhan Wuyao Pharmaceutical Co., Ltd.

The production of metronidazole is generally performed by batch tank reaction process with long-time and high-exhausting, accompanying with low conversion of the starting material 2-methyl-5-nitroimidazole and serious side-reaction of ethylene epoxide.A lot of waste acid and salt are generated in the productive process.Based on the original material and solvents, the reaction conditions were explored in single tube by the aid of a new tubular reactor.The results showed that the reaction could be quickly completed in 7-10 min at 90-95 °C.The reaction time was shortened by more than 30 times and the conversion of the nitro-compound was increased by 1.5 times.It suggests that a continuous production can be realized, and provides a tech. basis for the industrialization of metronidazole by tubular reaction.

One pot method is widely used in the synthesis of APIs.The traditional synthesis method of imatinib needs to prepare imatinic acid acyl chloride solid first, and then react with imatinic amime, which is not easy to operate in the production for the toxicity of acyl chloride.One pot method was used to solve the problem that acyl chloride was not easy to store and decomposeThe traditional two-step reaction was changed into one-step reaction, which simplified the operation steps, reduced the production cost and was more conducive to the process productionThe effects of the kinds of chlorination agents, the ratio of materials, the solvents and the temperature on the reaction were investigated.The optimum conditions for the synthesis of imatinib were obtained.

Bicalutamide tablets were prepared, comparing with the quality of reference list drug Casodex in laboratoryRelated substance was selected as evaluation of the types of adjuvant, the types of the disintegrating agent were confirmed through dissolution curve, the concentration of adhesive, the amount and the addition method of disintegrating agent and the amount of lubricant were studied through orthogonal design.The type of Opadry was researched through stress conditions.The final formulation can be used in pilot production