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    • 64. 发明申请
    • PROCESS FOR THE MANUFACTURE OF α-TOCOPHERYL ACETATE
    • 制备α-氯代醋酸酯的方法
    • WO2004063182A1
    • 2004-07-29
    • PCT/EP2003/014723
    • 2003-12-22
    • DSM IP ASSETS B.V.BONRATH, WernerDITTEL, ClausNETSCHER, ThomasPABST, ThomasGIRAUDI, Lisa
    • BONRATH, WernerDITTEL, ClausNETSCHER, ThomasPABST, ThomasGIRAUDI, Lisa
    • C07D311/72
    • C07D311/72
    • The present invention is concerned with a novel process for the manufacture of α-tocopheryl acetate which comprises reacting 2,3,6-trimethylhydroquinone-1-acetate with a compound selected from the group consisting of phytol (formula IV with R = OH), iso-phytol (formula III with R = OH), and (iso) phytol derivatives represented by the following formulae III and IV with R = C 2 -to C 5 -alkonoyloxy, benzoyloxy, mesyloxy, benzenesul-fonyloxy or tosyloxy, (IV) in the presence of a catalyst of the formula M n+ (R 1 SO 3 - ) n , wherein M n+ is a silver, copper, gallium, hafnium or rare earth metal cation, n is the valence of the cation M n+ , and R 1 is fluorine, C 1-8 -perfluoroalkyl or perfluoroaryl, and, if required, cyclizing any 3-phytyl-2,5,6-trimethylhydroquinone-1-acetate or a double bond isomer thereof obtained as an intermediate reaction product, to produce α-tocopheryl acetate. In the catalyst M n+ is preferably Ag + , Cu + , Ga 3+ , Sc 3+ , Lu 3+ , Ho 3+ , Tm 3+ , Yb 3+ or Hf 4+ .
    • 本发明涉及一种制备α-生育酚乙酸酯的新方法,其包括使2,3,6-三甲基氢醌-1-乙酸酯与选自植醇(式IV,R = OH)的化合物反应, 具有R = C 2〜C 5 - 烷酰氧基,苯甲酰氧基,甲磺酰氧基,苯并呋喃氧基或甲苯磺酰氧基的(Ⅳ)式(Ⅳ)所示的异构醇(式III与R = OH))和(异) 存在式M n +(R 1 SO 3 - )n的催化剂,其中M n +是银,铜,镓,铪或稀土金属阳离子,n是 阳离子M n +,R 1为氟,C 1-8 - 全氟烷基或全氟芳基,如果需要,可以将任何3-植酰基-2,5,6-三甲基氢醌-1-乙酸酯或其双键异构体环化为 中间体反应产物,以产生乙酸α-生育酚酯。 在催化剂中,M n +优选为Ag +,Cu +,Ga 3+,Sc 3+,Lu 3+,Ho 3+,Tm 3+,Yb 或者Hf <4+>。