申请人:Eisai Co., Ltd.
公开号:EP0658552A1
公开(公告)日:1995-06-21
A process is provided for the preparation of an α-tocopherol derivative represented by the following formula (VII):
wherein n stands for 0 or an integer of from 1 to 5. According to the process, trimethylhydroquinone and a particular allyl alcohol derivative or a specific alkenyl alcohol are subjected to a condensation reaction in the presence of a fluorosulfonate [M(RSO₃)₃], a nitrate [M(NO₃)₃] or a sulfate [M₂(SO₄)₃], wherein M represents a scandium, yttrium or lanthanide atom, and R represents a fluorine atom, a fluorinated lower alkyl group, or an aryl group which may be substituted by one or more fluorine atoms. The lanthanide atom means a lanthanum, cerium, praseodymium, neodymium, promethium, samarium, europium, gadolinium, terbium, dysprosium, holmium, erbium, thulium, ytterbium or lutetium atom.
提供了一种制备下式 (VII) 所代表的 α-生育酚衍生物的工艺:
其中 n 代表 0 或 1 至 5 的整数。根据该工艺,在氟磺酸盐[M(RSO₃)₃]存在下,三甲基对苯二酚和特定的烯丙基醇衍生物或特定的烯丙基醇发生缩合反应、硝酸盐[M(NO₃)₃]或硫酸盐[M₂(SO₄)₃],其中 M 代表钪、钇或镧原子,R 代表氟原子、氟化低级烷基或可被一个或多个氟原子取代的芳基。镧系原子是指镧、铈、镨、钕、钷、钐、铕、钆、铽、镝、钬、铒、铥、镱或镥原子。