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    • 5. 发明授权
    • Tocopherol derivatives and method for preparation thereof
    • 生育酚衍生物及其制备方法
    • US06410752B1
    • 2002-06-25
    • US09756179
    • 2001-01-09
    • Kil Joong KimDuck Hee KimHo Sik RhoJae Won YouChun Ja NamJong Eoun HongHak Hee KangIh Seob Chang
    • Kil Joong KimDuck Hee KimHo Sik RhoJae Won YouChun Ja NamJong Eoun HongHak Hee KangIh Seob Chang
    • C07F906
    • C07F9/65522A61K8/678A61Q19/08
    • 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.
    • 本发明的目的是提供由下式(I)表示的生育酚衍生物及其盐:其中,R1,R2和R3为H或甲基,以及至少一个选自R1 R2和R3位是甲基; 并且A是CH 2 -CH(CH 3) - 或CH = C(CH 3) - 本发明的另一个目的是提供一种制备上述生育酚衍生物的方法。 生育酚衍生物通过在有机碱存在下,在有机溶剂中使生育酚与磷酰氯以1:1〜1.3的当量比反应制备; 在有机溶剂中,通过上述反应生成的生育酚二氯磷酸与有机碱存在下的3-氨基丙醇反应; 并且水解上述产物。根据本发明的生育酚衍生物可以通过活体中的生物酶水解以产生生育酚和3-氨基丙烷磷酸酯。 它们可以诱导生理活性,包括恢复受伤的皮肤,防止生物膜老化等。此外,根据本发明的生育酚衍生物具有改善的稳定性,对皮肤的安全性和优于前述生育酚的抗氧化作用及其 衍生品