TOCOPHEROL DERIVATIVE AND PREPARING PROCESS THEREOF

摘要

PURPOSE: A tocopherol derivative and its preparing process are provided. The tocopherol derivative is stable and slowly releases tocopherol and 3-aminopropane phosphate, so that it can be used in a cosmetic composition. CONSTITUTION: The tocopherol derivative is represented by formula(I), in which R1, R2 and R3 are H or methyl; and A is CH2-CH(CH3)- or CH=C(CH3)-. The method for producing the tocopherol derivative comprises the steps of: reacting tocopherol with phosphorous oxychloride in the equivalent ratio of 1:1 to 1:1.3 in organic solvent in the presence of organic base at -10 to 50 deg.C for 1 to 3 hours to prepare tocopherol dichlorophosphate; reacting the tocopherol dichlorophosphate with 3-aminopropanol in organic solvent in the presence of organic base to prepare 2-tocopherol tetrahydro- 2H-1,3,2- oxazaphosphrin P-oxide; filtrating the 2-tocopherol tetrahydro- 2H-1,3,2- oxazaphosphrin P-oxide, adjusting the hydrogen concentration of the filtrated solution to pH 1 to 5, and reacting the filtrated solution at 5 to 100 deg.C for 1 to 10 hours; and extracting the produced tocopherol derivative with organic solvent and purifying it.