METHOD FOR PREPARING ARYL-CONDENSED POLYCYCLIC LACTAMS Russian patent published in 2007 - IPC C07D221/22 

FIELD: organic chemistry, chemical technology, medicine.

SUBSTANCE: invention relates to a method for synthesis of aryl-condensed polycyclic lactams of the formula (I) . Invention describes a method for synthesis of compound of the formula (I) wherein R¹ and R² are chosen independently from hydrogen atom, (C₁-C₅)-alkyl, (C₁-C₆)-alkoxy-group, trifluoromethyl, halogen atom, sulfonylalkyl, alkylamino-group, amide, ester, arylalkyl, heteroalkyl and arylalkoxy-group; or R¹ and R² in common with carbon atoms to which they are bound form mono- or bicycle; R³ represents (C₁-C₆)-alkyl. Method for synthesis of compound of the formula (I) involves the hydrogenation reaction of compound of the formula (II): with gaseous hydrogen and alcohol of the formula: R³-OH in the presence of a hydrogenation catalyst and acid wherein (a) hydrogenation catalyst comprises from about 5% to about 10% of palladium on carbon; (b) hydrogenation catalyst presents in the mass ratio of catalyst to compound of the formula (II) in the range from about 1:99 to about 10:90; (c) hydrogenation catalyst comprises from about 30% to about 60% of water as measured for mass; (d) nitrile group is subjected for reduction to the corresponding amino-group, and (e) acid presents in the equivalent ratio of acid to amino-group = about 1:1. Proposed method allows retaining stability of reactive aqua-labile the parent and intermediate compounds that results to the enhanced yield of the end product. Proposed method provides synthesis of polycyclic lactams of the formula (I) that can be used as intermediate substances in synthesis of condensed aryl azapolycyclic compounds representing medicinal agents used in treatment of neurological and psychic disorders.

EFFECT: improved method of synthesis, valuable medicinal properties of compounds.

11 cl, 2 ex