Cisatracurium besilate refining method

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The invention discloses a cisatracurium besilate finished product refining method. The cisatracurium besilate finished product refining method comprises the following steps: dissolving a cisatracurium besilate crude product in dichloromethane; putting the cisatracurium besilate crude product into purified water, adding benzenesulfonic acid, regulating pH value to be 1-5, adding the obtained solution into cisatracurium besilate dichloromethane solution, vigorously stirring, standing and removing a water layer, repeating the above steps for 1-7 times, and removing most water soluble impurities; adding a 4A molecular sieve into a dichloromethane layer, and fully drying while stirring; filtering the molecular sieve, controlling temperature, and dropwise adding ethyl acetate while stirring; removing the ethyl acetate, dissolving with dichloromethane, slowly dropwise adding the obtained solution into absolute ethyl ether with the weight 20-100 times of the weight of the obtained solution under the stirring condition, filtering the ethyl ether, and drying, so that the cisatracurium besilate finished product is obtained. The cisatracurium besilate finished product refining method has the advantages that cisatracurium besilate purification is improved, product quality is improved to some extent, and the defects of the original method that column chromatography needs to be carried out for purification when the product is unqualified and column chromatography is not applicable to quantization production, time-consuming and high in operation requirements can be overcome.

Public Papers of Nanjing University, "Shun music library synthesis and properties of ammonium research traitor" in said: atracurium besylate molecule has a chiral carbon atoms and one nitrogen atom chiral cis Atracurium is one of 10 kinds of isomers of atracurium. In this paper, tetrahydropapaverine as starting materials, N- acetyl -L- leucine as resolving agent, split to give R- tetrahydropapaverine N- acetyl -L- leucine salts, free too R- tetrahydropapaverine, and then refer to the preparation of acid atracurium same way, and pentamethylene diacrylate condensation condensate, and then into oxalate, refined, after free and benzenesulfonamide methyl ester was atracurium besylate, and finally by column chromatography to obtain ammonium acid sequence music library. Through the development of skeletal muscle relaxants and abroad a comprehensive evaluation study based on the successful development starting from domestic raw materials synthesis, split its chiral intermediates, optically active intermediates, until new technology and analysis along ammonium music library, in Control methods. And in accordance with the national "drug evaluation approach" to chemical synthesis and pharmaceutical nature of the research traitor, traitor systems preclinical research. The new process can be industrial production, synthesis of samples tested in full compliance with the standard drugs. First, review the nature and market muscle relaxant historical development, synthesis and structural changes, and muscle relaxants analysis. Second, to clarify the pharmacological activity of atracurium cis ammonium music library, and pharmacological activity of chiral drugs are described. Third, the synthesis and properties of cis ammonium study based music library.

benzenesulfonamide cis atracurium due to the unstable nature by column chromatography difficult to control, is to use its structure containing amino and carboxyl groups, and amino acids similar to the isoelectric point of a strong and stable characteristics, with acid water to remove water-soluble impurities, removing a portion of the fat-soluble impurities with ethyl acetate.