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US06410752B1 Tocopherol derivatives and method for preparation thereof 有权
生育酚衍生物及其制备方法

Tocopherol derivatives and method for preparation thereof
摘要:
An object of the present invention is to provide the tocopherol derivatives represented by the following formula (I), and their salts: Wherein, R1, R2 and R3 are H or methyl group, and at least one positions selected from group consisting of the R1, R2 and R3 positions are methyl group; and, A is CH2—CH(CH3)— or CH═C(CH3)— The other object of the present invention is to provide a method for preparing the above tocopherol derivatives. The tocopherol derivatives is prepared by reacting tocopherol with phosphorous oxychloride in an equivalent ratio of 1:1˜1.3, in presence of an organic base, in an organic solvent; reacting the tocopherol dichlorophosphate produced by the above reaction with 3-aminopropanol in presence of an organic base, in an organic solvent; and, hydrolyzing the above products. The tocopherol derivatives according to the present invention can be hydrolyzed by biological enzymes in a living body to produce tocopherol and 3-aminopropane phosphate. And they can induce physiological activities including recovery of injured skin, prevention from aging of bio-membrane, etc. Also, the tocopherol derivatives according to the present invention have improved stability, safety to skin and anti-oxidant effect superior to preceding tocopherol and its derivatives.
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