METHOD FOR PREPARING METHYLULPHATE NEOSTIGMINE AND IODIDE NEOSTIGMINE Russian patent published in 2012 - IPC C07C271/44 C07C269/06 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to chemistry and pharmaceutics, namely an improved method for preparing iodide or methylsulphate neostigmine which can find application as drugs. The method involves preparing sodium 3-dimethylaminophenolate, enabling its reaction with dimethylcarbamoyl acid chloride and reaction of prepared 3-((dimethylcarbomoyloxy)phenyl)-dimethylamine with an alkylating agent (iodomethane or dimethylsulphate). The method is characterised by the fact that target compounds are prepared by the reaction of 3-dimethylaminophenol with 2.0-2.5 molar excess of sodium metal in the toluene medium in boiling, addition of 1.5 molar excess of dimethylcarbamoyl acid chloride, washing out of the toluene filtrate with a sodium alkali solution and water, evaporation of a solvent and keeping of 3-((dimethylcarbomoyloxy)phenyl)-dimethylamine with the relevant alkylating agent for 24 hours in the absolute diethyl ester medium.

EFFECT: method enhancing the 3-dimethylaminophenol conversion, as well as providing higher yield and purity of the end product.

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