METHOD OF PRODUCING 4-PENTAFLUOROSULFANYL BENZOYL GUANIDINES Russian patent published in 2010 - IPC C07C381/00 

FIELD: chemistry.

SUBSTANCE: invention relates to a method of producing 4-pentafluorosulfanyl benzoyl guanidines of formula which are NHE-1 inhibitors, where R1 is hydrogen, R2 is alkyl with 1-6 carbon atoms, R3 and R4 represent hydrogen, in which a) a derivative of sulphur 4-nitrophenylpentafluoride of formula II is reduced to obtain an amine of formula III, and b) the formula III compound in the ortho-position of the amino group is halogenated using a halogen-containing agent to obtain a compound of formula IV, and c) using a suitable nucleophile or organoelemental compound, for example a boron alkyl compound, under catalysis conditions if necessary, the halogen substitute in the formula IV compound is substituted with a substitute R2, and d) in the formula V compound, the amino group is substituted with a halogen substitute, and e) in the formula VI compound, the halogen substitute is substituted with a nitrile group, and f) the nitrile group in formula VII compound is hydrolysed to obtain a carboxylic acid, and g) the carboxylic acid of formula VIII is converted to acylguanidine of formula I; and intermediate compounds of formula X and formula XI which are intermediate compounds in synthesis of formula I compounds.

EFFECT: possibility of obtaining formula I compounds from commercially available raw material and high output of end product.

6 cl, 1 ex