SELECTIVE METHOD FOR PREPARATION OF ENANTIOMERS OF HYDROXYWILFORDIC ACID AND ESTER DERIVADIVES THEREOF

摘要

PURPOSE: A method for selectively preparing enantiomers of hydroxy wilfordic acid and ester derivatives thereof is provided to develop anti-HIV agents and physiologically active materials. CONSTITUTION: A method for preparing hydroxy wilfordic acid of chemical formula 1 or an ester derivative of chemical formula 2 comprises the steps of: increasing carbons in a pyridine derivative of chemical formula 4 and preparing an alpha, beta-unsaturated ketone derivative of chemical formula 5; performing cyanosilylation of the derivative of chemical formula 5 under the presence of a cyano reagent and an organic catalyst to prepare a trimethylsilyl cyanohydrin derivative of chemical formula 6; hydrolyzing and esterifying the derivative of chemical formula 6 and preparing a compound of chemical formula 9; and adding Pd/C to the compound of chemical formula 9 and reducing the compound of chemical formula 9 under the presence of hydrogen gas.