METHODS FOR PREPARING SUBSTITUTED ARYL-CONDENSED AZAPOLYCYCLIC COMPOUNDS, INTERMEDIATE SUBSTANCES AND METHODS FOR THEIR PREPARING Russian patent published in 2006 - IPC C07C255/47 C07C253/30 C07C229/50 C07C227/06 C07D221/22 C07D317/30 C07D319/06 

FIELD: organic chemistry, chemical technology, medicine.

SUBSTANCE: invention relates to a new method for synthesis of substituted aryl-condensed azapolycyclic compounds of formulas (II) and (VIII) , novel intermediates compounds and methods for their synthesis. Substituted aryl-condensed azapolycyclic compound of the formula (II) show the binding capacity with neurone nicotine/acetylcholine specific receptor sites and can be used for modulation of cholinergic function in treatment of different diseases. Method for synthesis of compound of the formula (II) wherein R represents hydrogen atom; R² and R³ are chosen independently from hydrogen, halogen atom, (C₁-C₆)-alkyl optionally substituted with 1-3 fluorine atoms and (C₁-C₆)-alkoxy-group optionally substituted with 1-3 fluorine atom involves the hydrogenation reaction of compound of the formula: (1a'): synthesized from compound of the formula (III): to yield intermediate compounds of formulas (IX): and (VII): . Compound of the formula (VII) is cyclized in treatment with a base to yield compound of the formula (VIII) that is reduced. Compound of the formula (III) can be prepared by interaction of compound of the formula (IV): with compound of the formula (V): .

EFFECT: improved methods of synthesis.

14 cl, 12 sch, 64 ex