PROLINE DERIVATIVES USEFUL FOR TREATMENT OF SKIN DISEASE, COSMETIC COMPOSITION COMPRISING THE SAME AND PREPARING METHOD THEREOF

摘要

PURPOSE: Proline derivatives, a cosmetic composition comprising the same and a preparing method thereof are provided. The derivatives have non-stimulation property, improved collagen synthesis and antioxidative activities, and improved UV and heat stabilities. Therefore, they can be useful for treatment of skin disease such as sensitive skin, atopic dermatitis and psoriasis. CONSTITUTION: The proline derivative is represented by the formula(1), wherein R1, R2 and R3 are hydrogen simultaneously, or other two of them are hydrogen when one of them is hydroxy; and R4 and R5 are hydrogen or methyl. The cosmetic composition comprises 0.01 to 20 wt.% of the proline derivative represented by the formula(1). The method for preparing the proline derivative represented by the formula(1) comprises the steps of: (i) reacting a compound of the formula(2) with benzylchloro formate of the formula(3) in the solvent; (ii) reacting the product of the step (i) with tocopherol of the formula(5) in the solvent in the presence of catalyst to prepare a compound of the formula(6); (iii) bubbling reacting the compound of the formula(6) under hydrogen gas at room temperature to isolate benzyl chloroformate; and (iv) filtering and concentrating the benzyl chloroformate.