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    • 3. 发明公开
    • 1,4-디페닐 아제티딘온 유도체의 제조방법
    • 生产1,4-二苯基亚乙基二酮衍生物的方法
    • KR1020070027554A
    • 2007-03-09
    • KR1020067024431
    • 2005-05-20
    • 사노피-아벤티스 도이칠란트 게엠베하
    • 린덴슈미트안드레아스윌데이비드윌리암야에네게르하르트볼만테오도르안드레아스프리크벤델린윤커베른트리갈데이비드빌렌귄터옌드랄라하이너
    • C07D205/08
    • C07D205/08A61K31/33
    • The invention relates to a method for producing 1,4-diphenyl azetidinone derivatives from suitably protected beta-substituted amino amides, in the presence of silylation agents. Said method uses cyclization catalysts that comprise phosphonium ions as the cation of formula (XII), and ions of the following general formulas (a), (b), (c) or (d) as the anion. In said formulas, the symbols, substituents and indices are defined as follows: Z = C=O, C=S, S=O, SO2 or C=NR20; K = O, S, NR21 or CR22R23; L = NR24 or CR25R26; n = 0 or 1; M = O, C=O, NR27 or CR28R29; Q = O, S, NR30, CR31R32,C=O, C=S, S=O, SO2 or C=NR34; R = CR35 or N; T = CR36 or N; U = CR37 or N; V = CR38 or N; the groups R16 to R19can represent, for example, aryl or (C1-C15) alkyl, aryl(C1-C10)alkene, and the groups R20 to R32 and R34 to R38 can represent in addition H or heteroaryl; R39 and R40 represent, for example (C1-C6) alkyl. The anion can also be R41O-,R42COO- or Cl-, Br- or I- (combined with Ag2O). ® KIPO & WIPO 2007
    • 本发明涉及一种在甲硅烷基化剂存在下从适当保护的β-取代氨基酰胺生产1,4-二苯基氮杂环丁酮衍生物的方法。 所述方法使用包含鏻离子作为式(Ⅻ)的阳离子和以下通式(a),(b),(c)或(d)的离子作为阴离子的环化催化剂。 在所述式中,符号,取代基和指数定义如下:Z = C = O,C = S,S = O,SO 2或C = NR 20; K = O,S,NR21或CR22R23; L = NR24或CR25R26; n = 0或1; M = O,C = O,NR 27或CR 28 R 29; Q = O,S,NR30,CR31R32,C = O,C = S,S = O,SO2或C = NR34; R = CR35或N; T = CR36或N; U = CR37或N; V = CR38或N; 基团R16至R19可以表示例如芳基或(C1-C15)烷基,芳基(C1-C10)烯基,并且基团R20至R32和R34至R38可以另外表示H或杂芳基; R 39和R 40表示例如(C 1 -C 6)烷基。 阴离子也可以是R41O-,R42COO-或Cl-,Br-或I-(与Ag2O结合)。 ®KIPO&WIPO 2007