METHOD OF PRODUCING (3-OXO-2,3-DIHYDRO-1H-ISOINDOL-1-YL)-ACETYLGUANIDINE DERIVATIVES Russian patent published in 2010 - IPC C07D209/46 C07C233/66 

FIELD: chemistry.

SUBSTANCE: invention relates to a method of producing compounds of formula I , where R1 and R2 independently denote H, F, CI, OCF₃, 2,2,2-trifluoroethoxy, -CF₃, 2,2,2-trifluoroethyl, C1-C4alkyl; R3 denotes Alk-R4, -CF₃; Alk denotes C1-C4alkyl; R4 denotes H, -CF₃, C3-C7cycloalkyl; as well as their pharmaceutically compatible salts, distinguished by that, as defined on figure 1: a) an amide of formula IV is formylated in the ortho position to an amide group and then, without extraction of the obtained intermediate compound, cyclised to obtain a compound of formula IV, b) the formula IV compound is converted with alkoxycarbonyl methylene triphenylphosphorane, with 1-alkoxy-1-trimethylsiloxy ethylene or with trialkylphosphonoacetate to obtain a formula VII compound, and c) converting the formula VII compound with guanidine to obtain a formula I compound, where in formula IV-VII compounds R1-R3 are as defined in formula I; R5 is -OC1-C4alkoxy. Intermediate compounds and a racemic separation method are described.

EFFECT: design of an efficient method of producing compounds.

15 cl, 4 dwg, 7 ex