发明授权
EP1430018B1 VERFAHREN ZUR HERSTELLUNG VON BETA-ALANINAMIDEN 有权
PROCESS FOR BETA-ALANINAMIDEN的制备

  • 专利标题: VERFAHREN ZUR HERSTELLUNG VON BETA-ALANINAMIDEN
  • 专利标题(英): Method for producing beta-alanine amides
  • 专利标题(中): PROCESS FOR BETA-ALANINAMIDEN的制备
  • 申请号: EP02767473.8
    申请日: 2002-09-04
  • 公开(公告)号: EP1430018B1
    公开(公告)日: 2010-12-29
  • 发明人: HANSELMANN, PaulHILDBRAND, Stefan
  • 申请人: Lonza AG
  • 申请人地址: Münchensteinerstrasse 38 4052 Basel CH
  • 专利权人: Lonza AG
  • 当前专利权人: Lonza AG
  • 当前专利权人地址: Münchensteinerstrasse 38 4052 Basel CH
  • 优先权: EP01121342 20010906; US332547P 20011126
  • 国际公布: WO2003022795 20030320
  • 主分类号: C07C209/48
  • IPC分类号: C07C209/48 C07C279/14 C07C237/02 C07D239/20
VERFAHREN ZUR HERSTELLUNG VON BETA-ALANINAMIDEN
摘要:
The invention relates to β-alanine amides of general formula (I), wherein: R1 represents hydrogen or C¿1-6? alkyl that is optionally substituted by hydroxy, amino, carboxy, carbamoyl, methylmercapto, guanidino, optionally substituted aryl or heteroaryl, and; R?2¿ represents hydrogen or R?1 and R2¿, together, form a group of formula -(CH¿2?)n-, wherein n is 3 or 4. Said β-alanine amides are produced without using an amino protective group by reacting the corresponding amine with a cyanoacetic ester in order to form an acetamide and by effecting a subsequent catalytic hydrogenation. The method is suited, in particular, for producing carcinine (β-alanyl-histamine, R?1 ¿= imidazol-4-ylmethyl, R2 = H), a naturally occurring pseudo dipeptide, which is used as an active ingredient having an antioxidative effect in medicaments and cosmetics.
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