| 摘要 |
FIELD: chemistry; pharmacology. ^ SUBSTANCE: method involves production of N-substituted 3beta-aminonortropanes of formula I or one of acid-additive salts , where R1 represents optionally substituted residue chosen from group, including C1-C8alkyl, C2-C8alkenyl, C3-C8cycloalkyl and C6-C10aryl-C1-C8alkyl, characterised that either a) related 3-oxonortropane of formula IIA reacts with arylmethylamine of formula IIIA H2N-CH2-Ar (IIIA) where Ar stands for optionally substituted phenyl residue or optionally substituted 5 or 6-merous heteroaromatic residue with at least one heteroatom chosen from group including N, O and S, or b) related 3alpha-aminonortropane of formula IIB reacts with arylaldehyde of formula IIIB O-CH-Ar (IIIB). Produced in each case imine of formula IVA or IVB is transformed to thermodynamically stable tautomer, respectively isomer of formula V , then hydrolysed and if required transformed to related acid-additive salt. ^ EFFECT: produced compounds of formula I are valuable intermediate in chemical synthesis of various pharmaceutical reactants or represent pharmaceutical reactant, first of all as NMDA-receptor modulators; method allows for high-yield commercial production of high-purity 3-aminonortropanes. ^ 9 cl, 4 ex |
