| 摘要 |
FIELD: organic chemistry, chemical technology, medicine, ophthalmology. ^ SUBSTANCE: invention relates to a new method for synthesis of 5-bromo-6-[(2-imidazolin-2-yl)amino]quinoxaline L-tartrate (brimonidine L-tartrate) of the formula (I): that is a highly effective medicinal agent used in glaucoma treatment. Method involves condensation of N,N-dimethyldichloromethylene immonium chloride of the formula: (CH3)2N+=CCl2Cl- with 5-bromo-6-aminoquinoxaline in organic solvent medium followed by treatment with ethylenediamine of formed N,N-dimethyl-N1-(5-bromoquinoxalin-6-yl)-alpha-chloroformamidine of the formula: RN=C(Cl)N(CH3)2 wherein R means 5-bromoquinoxalin-6-yl. Synthesized intermediate compound is extracted from reaction and mass and subjected for cyclization to 5-bromo-6-[(2-imidazolin-2-yl)amino]quinoxaline that is converted to L-tartrate by interaction with L-tartaric acid in acetone medium. Invention provides simplifying the technological process that is carried out under mild conditions and without isolation of intermediate substances that allows preparing the end preparation with the high yield about 40% as measure for 5-bromo-6-aminoquinoxaline. ^ EFFECT: improved method of synthesis. ^ 1 cl, 2 ex |
