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

Summary
New optimized chemocatalytic route for important precursors N-acyl-α-aminonitriles or N-sulfonyl-α-aminonitriles, e.g. of Vildagliptin® or Saxagliptin®.
Technology Benefits
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
Technology Application
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
Detailed Technology Description
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
Type of Cooperation
Licensing
Application Date
17/08/2017 00:00:00
Application No.
DE201610116130 20160830
Classes
- international:
C07C253/00; C07C255/32; C07D207/16; C07D209/52
- cooperative:
C07B51/00; C07D207/16; C07B2200/07
Others
Patent application
ID No.
4654
Country/Region
Germany

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