SYNTHESIS OF SUBSTITUTED PYRAZOLINE CARBOXAMIDINE DERIVATIVES Russian patent published in 2015 - IPC C07D231/06 C07D231/54 C07D403/12 C07D409/04 C07D409/12 C07D491/107 

FIELD: chemistry.

SUBSTANCE: invention relates to a method of producing pyrazoline carboxamidine derivatives of formula . Said compounds are known as powerful 5-HT₆ antagonists. The disclosed method comprises reacting a corresponding substituted 4,5-dihydro-(1H)-pyrazole or an isomer thereof with isothiocyanate R₆-N=C=S to obtain an amide of substituted 4,5-dihydro-(1H)-pyrazole-1-carbothioic acid or tautomeric substituted 4,5-dihydro-(1H)-pyrazole-1-carboxymidothioic acid . The obtained intermediate compounds are reacted with a corresponding alkylating agent to obtain an intermediate S-alkylated compound . Said intermediate compound is reacted with a sulphonamide derivative R₇SO₂NH₂ and the target compound of formula (I) is separated from the reaction mixture. The invention also relates to novel intermediate products (III^a), (III^b) and (IV). Symbols given in the formulae have values given in the description.

EFFECT: providing an alternative method which improves atom efficiency of synthesis of desired compounds with higher output compared to existing methods for synthesis of said compounds.

8 cl, 1 tbl, 3 ex