5 - amino - 2,4,6 - the triode - 1,3 - the method of producing the benzene di-carboxylic acid derivative

摘要

(57) Abstract This invention is the derivative of 5- amino -1,3- benzene di-carboxylic acid, hydroxyl is the method of producing the non ionicity iodic conversion contrast medium which possesses the acyl amino residue which is substituted in 5 rank, every intermediate field without being isolated, it regards the method of including the below-mentioned process: Reacting with the acyl chloride which possesses the hydroxyl basis which is protected (a) 5- amino -2,4,6- triode -1,3- benzenjikarubonjikurorido, as ester, the process which obtains the solution of the 5- acyl amino -2,4,6- triode -1,3- benzene di-carboxylic acid dichloride in dimethyl acetamide; (B) in the not yet refinement solution which from process (a) is obtained, formula: The tertiary amine which with NR₁ R₂ R₃ (in formula, R₁, R₂, as for R₃, becoming independent, (C₁ - C₁₂) direct condition or the divergence condition alkyl group, (C₁ - C₃) the alkyl (C₆ - C₁₀) aryl basis or (being C₁ - C₄) arukeniru bases,) is shown, while maintaining reaction temperature at 0 - the 30C, the process which it adds at 3 - 15% quantity vis-a-vis the mol quantity of the acyl chloride; (C) process (b) from in the solution which is obtained, N which corresponds including amino alcohol, N'- bis (2,4,6- triode -1,3- benzenjikarubokisamido) profit, adding water disassembling this directly, the process which deviation from protects the hydroxyl basis which is protected.