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    • 9. 发明授权
    • Process for the allylation of n-acylhydrazones
    • N-酰基腙的烯丙基化方法
    • US07659424B2
    • 2010-02-09
    • US10591094
    • 2005-02-24
    • Shu KobayashiMasaharu Sugiura
    • Shu KobayashiMasaharu Sugiura
    • C07C241/02C07C227/04C07C229/08C07C243/38
    • C07C241/02C07B53/00C07C2601/14C07C243/38
    • [PROBLEMS] To provide a novel method for the allylation of N-acylhydrazones by which enantioselectively allylated N-acylhydrazines can be efficiently obtained.[MEANS FOR SOLVING PROBLEMS] A method for the production of enantioselectively allylated N-acylhydrazines represented by the general formula [3]: [wherein R0 is an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group, or —COOR1 (wherein R1 is a hydrocarbon group); R2 is acyl; R3 and R4 are each hydrogen, or one of R3 and R4 is hydrogen and the other is a hydrocarbon group; and R5 and R6 are each independently hydrogen or a hydrocarbon group], characterized by reacting an N-acylhydrazone represented by the general formula [1]: [wherein R0 and R2 are as defined above] with an allylating agent such as allyltrichlorosilane or crotyltrichlorosilane in the presence of a chiral phosphine oxide.
    • [问题]提供N-酰腙的烯丙基化的新方法,通过该方法可以有效地获得对映选择性烯丙化的N-酰肼。 用于解决问题的方法制备由通式[3]表示的对映选择性烯丙化N-酰肼的方法:[其中R 0是任选取代的烃基,任选取代的杂环基或-COOR 1(其中R 1是 烃基); R2是酰基; R3和R4各自为氢,R3和R4中的一个为氢,另一个为烃基; R 5和R 6各自独立地为氢或烃基],其特征在于使由通式[1]表示的N-酰腙:[其中R 0和R 2如上定义]与烯丙基化试剂如烯丙基三氯硅烷或基环丙基三氯硅烷反应 存在手性氧化膦。