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

FIELD: organic chemistry. SUBSTANCE: invention relates to a compound of the formula (I) where stereocenter α has R- or S-configuration or it is racemic; r - a whole number from 0 to 5; R¹, R² - hydrogen atom, alkyl; or R¹ and R² in common with nitrogen atom to which R¹ is bound and carbon atom to which R² is bound form 3-10-membered monocyclic saturated ring system involving nitrogen atom, 1-8 carbon atoms and one heteroatom of the formula =N-V-R¹ where V is absent or means COO- or = N-COO-benzyl or = N-CH₂-pyridyl; R³ - H, C_1-4-alkyl, C_2-10-cycloalkyl, C_6-10-nonsubstituted aryl and pyridyl; R⁴ is C_1-5-alkyl. Compounds are synthesized by interaction of the compound of the formula (II) and formula (III) in the presence of a strong base at low temperature. The method shows high degree of diastereoselectivity, does not use toxic reagents. EFFECT: decreased time of synthesis. 29 cl, 19 ex