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Method for chemical production of enantiomerically pure chiral N-Acyl-a-aminonitriles

总结: New optimized chemocatalytic route for important precursors N-acyl-α-aminonitriles or N-sulfonyl-α-aminonitriles, e.g. of Vildagliptin® or Saxagliptin®.

技术优势: Effective chemical production process of N-acyl-a-aminonitriles or N-sulfonyl-a-aminonitriles
Enantiomerically pure Gliptin derivatives
New optimized chemocatalytic route
New approach for important precursors, e.g., of Vildagliptin® or Saxagliptin®
Starting material easy accessible and avoiding cyanide or Vilsmeier reagents as toxic reagents

技术应用: Enantiomerically pure N-acyl--aminonitriles gained these days interest in the
pharmaceutical industry since a range of recently developed pharmaceuticals are
based on this product class. Examples are Vildagliptin®, Saxagliptin® or
NVP-DPP-728, which are active pharmaceutical ingredients against diabetes type II

详细技术说明: Important precursors of are synthesized via multiple phase reactions as state of the art and typical strategies towards such types of molecules are based on toxic reagents such as cyanides or Vilsmeier reagents. The
production of the latter one includes toxic precursors like oxalylchloride and
phosphorylchloride. The present invention focuses on a production process which avoids the need of such toxic reagents. In addition, it has the advantage that the reaction can be conducted under mild conditions

分类: - international:
C07C253/00; C07C255/32; C07D207/16; C07D209/52
- cooperative:
C07B51/00; C07D207/16; C07B2200/07

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