HYDROCHLORIDES OF SUBSTITUTED ACETYLENIC AMINOALCOHOL-ACTIVE AND LOW-TOXIC HALOPERIDOL ANTAGONISTS

摘要

medicine. SUBSTANCE: described are new substituted acetylenic aminoalcohol hydrochlorides of general formula 1 R1R2C(OH)CH2C=CCH2Am.HCl which have low toxicity and have properties of haloperidol antagonists which are useful in medicine for treatment and prophylaxis of parkinsonism. In general formula 1 R1,R2 and Am are as defined in 1a: C6H5, cyclopentyl, N[CH(CH3)2]2; 1b: C6H5, cyclopentyl, pyrrolidino; 1c: C6H5, cyclopentyl, piperidono; 1d: cyclopentyl, C6H5,N(CH2CH3)2; 1e: cyclopentyl, C6H5, pyrrolidino; 1f: R1 and R2 together form group A; Am is ; 1g: N(CH2CH3)2 and R1 and R2 together form said group A, and Am is pyrrolidino. Compounds are prepared using Mannich reaction by reacting corresponding amino compound and acetylenic alcohol in the presence of copper salts. EFFECT: improved properties of compounds. 2 tbl