Retinol derivatives, the method of preparations and the uses thereof

A retinol derivative comprising a carboester linkage between retinol and an amino acid said retinol derivative having formula (II):

• wherein:
• R1 is H, CHO, retinoic acid, acetate or tert-butoxycarbonyl;
• R2 is OH, OCH3, OC2H5, retinol or conjugated linoleic acid;
• and
• n is the integer of 1–6.

A method for preparing retinol carboester derivative comprising the steps of:

• (1) obtaining pure retinol by:
• a) combining of retinyl acetate with an inorganic salt in a methanolic solvent;
• b) extracting of a product of step 1a by an ether solvent;
• (2) obtaining retinol carboester derivatives by:
• a) combining a compound selected from the group consisting of a peptide selected from the group consisting of di-, tri- and polypeptide comprising α-aspartyl-L-phenylalanine-1-methylester(APM;
• aspartam), N-protecting group-aspartam and neotam, an amino acid having two carboxyl groups, a moiety having carboxyl group and multiple double bonds on a carbon chain and a moiety having two carboxyl groups and one double bond on a carbon chain, with a condensing agent and methylene chloride to activate the acidity of the selected compound;
• b) adding retinol to the reaction mixture of step 2a in the presence of a catalyzing agent;
• and
• (3) separating obtained retinol carboester derivatives by column chromatography using a silicagel.