METHOD OF SYNTHESIS OF N-[2-(DIMETHYLAMINO)-ETHYL]-ACRIDINE-4- - CARBOXAMIDE AND ITS DERIVATIVES Russian patent published in 2002 - IPC

FIELD: organic chemistry, chemical technology, pharmacy. SUBSTANCE: invention relates to a novel method of synthesis of acridine carboxamide of the formula (I) where R¹,R²,R⁵,R⁶, x, Y are indicated in the invention claim. Method of synthesis involves cyclization of compound of the formula (II) by treatment with boron trifluoride or suitable complex based on its in a suitable solvent to yield tetrafluoroborate salt of the formula (IIIa) followed by treatment of this salt with inorganic base in EtOAc or CH₂Cl₂ medium to form compound of the formula (III) and treatment of: (i) compound of the formula (III) with primary alkyl amine of the formula (IV) NH₂(CH₂)_xY (IV) or (ii) carboxylic acid obtained by hydrolysis of compound of the formula (III) at alkaline conditions with primary alkyl amine of the formula (IV) in the presence of a suitable binding agent to yield compound (I) or if necessary the conversion of one compound of the formula (I) to other compound of the formula (I) and/or to its pharmaceutically acceptable salt. Invention provides to synthesize the useful compound which is an antitumor medicinal agent, easy separation and further processing tetrafluoroborate salt. EFFECT: new improved method of synthesis, simplified process in industrial scale, increased productivity of process, valuable antitumor properties of compound. 8 cl, 12 ex