INTERMEDIATE COMPOUNDS FOR SYNTHESIS OF HIV-PROTEASE INHIBITORS AND A METHOD OF THEIR SYNTHESIS Russian patent published in 1999 - IPC

FIELD: organic chemistry. SUBSTANCE: invention relates to new intermediate compounds that inhibit activity of protease encoded by HIV, in part, L-735524, or to their pharmaceutically acceptable salts. Method of synthesis derivatives of heterocyclic carboxylic acids of the formula (I) involves interaction of a compound of the formula (IV) with amine of the formula (V) where stereocenter "a" has R- or S-configuration, or it is racemic; r = 0-5; R¹ and R² taken together with nitrogen atom to which R¹ is bound and carbon atom to which R² is bound form 6-membered monocyclic saturated ring system. The latter consists of nitrogen atom to which R¹ is bound, 4 carbon atoms and one substituted heteroatom where R^a means alkyl; R³ - phenyl; R⁴ - C_1-5-alkyl. EFFECT: improved method of synthesis, increased yield, enhanced stereospecificity, simplified method. 20 cl