INTERMEDIATE COMPOUND OF GADOBUTROL AND METHOD OF PRODUCING GADOBUTROL USING SAID INTERMEDIATE COMPOUND Russian patent published in 2021 - IPC C07D257/02 C07F5/00 

FIELD: chemistry.

SUBSTANCE: invention relates to a method of producing gadobutrol, which involves reacting 1,4,7,10-tetraazacyclododecane with a lithium-halogen salt to form a cyclo-lithium halogen complex with subsequent reaction with 4,4-dimethyl-3,5,8-trioxabicyclo[5.1.0]octane at temperature from 85 to 95 °C to obtain a complex of N-(6-hydroxy-2,2-dimethyl-1,3-dioxyphen-5-yl)-1,4,7,10-tetraazacyclododecane-lithium halogen, represented by following chemical formula 1 (where X is halogen); reaction of a lithium halogen complex represented by chemical formula 1, with hydrochloric acid to obtain an intermediate compound of gadobutrol, represented by the following chemical formula 2; alkylation of an intermediate compound of gadobutrol represented by the following chemical formula 2 with chloroacetic acid to obtain a butrolrol of the following chemical formula 3; and reacting the butrolene represented by chemical formula 3 with gadolinium oxide.

Chemical formula 1

Chemical formula 2

Chemical formula 3

EFFECT: technical result is a new method of obtaining high purity gadobutrol, which is used in medicine as a contrast agent for MRI.

1 cl, 2 ex