The Study On The Synthesis Technology Of Closantel Aodium

Closantel Sodium,a kind of high efficiency,low toxicity and broad-spectrum deworming drugs which have enjoyed a high reputation in the international market,can be used for the treatment and prevention of cattle,sheep parasitic infections.Its mechanism of action and application fields consistent with closantel.China's ministry of agriculture issued closantel as a new drug in 1993.There are few report of the domestic synthesis about closantel sodium.The thesis introduces the synthesis conditions of closantel sodium,and the expandable production experiment based on the optimization of process conditions,The thesis consists of three parts.In the first part,the physicochemical,pharmacological properties,clinical application and drug security of closantel sodium were introduced.And the existing synthetic methods of closantel sodium,the type of metal catalysts and application fields were also introduced.In the second part,we studied on the synthetic process of closantel sodium.We improved a synthetic route to closantel sodium starting from p-chlorobenzyl cyanide and 4-Chloro-2-nitro toluene by condensation,hydrogenation reduction,amidation and salt forming reaction.We optimized the catalytic reduction reaction and amidation reaction which were the key step in the synthesis of closantel sodium.First palladium carbon was used as catalyst in the hydrogenation reduction.Second the replace of amidation reagent was researched,adopting low toxicity bis(trichloromethyl)carbonate instead of phosphorus trichloride.Our method owned the character of concise procedures,good yields and mild reaction conditions.In the three part,according to the optimization of process conditions,we studied the amplification and trial production experiments,investigated the stability of process.The yield was relatively stable,this synthetic routes have industrialization prospect.