METHOD OF SYNTHESIS OF INTERMEDIATE COMPOUNDS USED FOR SYNTHESIS OF HIV-PROTEASE INHIBITORS

摘要

FIELD: organic chemistry. SUBSTANCE: invention relates to a compound of the formula (I) where stereocenter alpha has R- or S-configuration or it is racemic; r - a whole number from 0 to 5; R1, R - hydrogen atom, alkyl; or R and R in common with nitrogen atom to which R is bound and carbon atom to which R 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-R where V is absent or means COO- or = N-COO-benzyl or = N-CH2-pyridyl; R - H, C1-4-alkyl, C2-10-cycloalkyl, C6-10-nonsubstituted aryl and pyridyl; R is C1-5-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