NOVEL RETINOL DERIVATIVE, METHOD FOR PREPARING THE SAME AND USES THEREOF

摘要

PURPOSE: Provided are a novel retinol derivative, its preparation method in higher yield, and its use. The novel retinol has excellent light-stability, and shows high reactivity to retinoic acid receptor α, while showing low reactivity to retinoic receptor β and γ. It can applied to medical products, cosmetics, soap, shampoo, functional foods, etc., for the prevention and improvement of skin aging. CONSTITUTION: The novel retinol derivative is characterized by carboester bond of a peptide material having COOH group, wherein the peptide material having COOH group is selected from -di, -tri, -poly peptide including N-L- α-aspartyl-L-phenylalanine 1-methylester(AMP;aspartame), N-protection group-aspartame, neotame and the like. Its manufacturing method comprises the steps of: reacting retinylacetate with methanolic solvent and inorganic slat at 25-40 deg.C in a dark room then extracting the reaction product with ether solvent; removing the solvent then followed by mixing a compound having OH group, natural or separated and purified retinol, diethylazodicarboxylate and triphenylphosphate with methylenechloride solvent, and reacting them at room temperature to obtain the ester derivative of retinol; and performing chromatography with reverse-phase, Merck Silicagel 60 RP 18(40-63) micro meter to separate pure ester derivative of retinol.