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    • 2. 发明公开
    • Process for preparing 1,5-benzothiazepine derivatives
    • Verfahren zur Herstellung von 1,5-Benzothiazepinderivaten。
    • EP0395302A1
    • 1990-10-31
    • EP90304200.0
    • 1990-04-20
    • TANABE SEIYAKU CO., LTD.
    • Nishimoto, ShigeruNakao, AkioIkeda, YasujiNate, Hiroyuki
    • C07D281/10
    • C07D281/10
    • There is disclosed a process for preparing 1,5-benzothiaze­pine derivatives represented by the formula:
      wherein one of R¹ and R² is a lower alkyl group or halogen atom, and the other is hydrogen atom, R³ is a lower alkyl group or a lower alkoxy group,
      which comprises subjecting a propionic acid compound represented by the formula (II):
      wherein R¹, R² and R³ have the same meanings as defined above, and R⁴ represents hydrogen atom or an ester residue,
      to intramolecular ring closing reaction in the presence of a sulfonic acid compound represented by the formula (III):
      R⁵SO₃H      (III)
      wherein R⁵ represents a lower alkyl group or a sub­stituted or unsubstituted phenyl group.
    • 公开了一种制备由下式表示的1,5-苯并硫氮杂衍生物的方法:其中R 1和R 2之一为低级烷基或卤素原子,另一个为氢原子,R 3是低级烷基或低级烷氧基,它包括使由式(Ⅱ)代表的丙酸化合物:其中R 1,R 2和R 3具有相同的 在式(III)表示的磺酸化合物的存在下,R 4表示氢原子或酯残基至分子内闭环反应:R 5 SO 3 H(III)其中R 1, 5“表示低级烷基或取代或未取代的苯基。