Con esta herramienta te facilitamos un acceso a todas las ofertas y demandas de tecnología europeas y a búsquedas de socios para participar en propuestas europeas de I+D publicadas en la red Enterprise Europe Network, pudiendo filtrar los resultados para facilitar las búsquedas más acordes con tus necesidades.

¿Quieres recibir estos listados de oportunidades de colaboración en tu correo de forma periódica y personalizada? Date de alta en nuestro Boletín

Los términos de búsqueda han de ser en inglés.

N-Acil-alfa-aminonitrilos quirales enantioméricamente puros

Resumen

Tipo:
Oferta Tecnológica
Referencia:
TODE20161110001
Publicado:
30/11/2016
Caducidad:
30/11/2017
Resumen:
Una universidad alemana ha desarrollado un nuevo método para la producción química de N-acil-a-aminonitrilos enantioméricamente puros o N-sulfonil-a-aminonitrilos, activos como ingredientes farmacéuticos contra la diabetes tipo 2. Este método no necesita reactivos tóxicos y presenta otras ventajas: derivados de gliptina enantioméricamente puros, nueva ruta quimiocatalítica optimizada, nuevo enfoque para precursores importantes, por ejemplo, de Vildagliptin® o Saxagliptin® y material de base accesible evitando reactivos tóxicos. La universidad busca socios industriales con el fin de establecer acuerdos de licencia y cooperación técnica.


Details

Tittle:
Enantiomerically pure chiral N-Acyl-alpha-aminonitriles
Summary:
A German university developed a novel method for the chemical production of enantiomerically pure chiral N-acyl-a-aminonitriles or N-sulfonyl-a-aminonitriles, active in pharmaceutical ingredients against diabetes type 2. The method does not need toxic reagents. The university offers a license agreement as well as a technical cooperation agreement to industrial partners.
Description:
Enantiomerically pure N-acyl-a-aminonitriles have gained interest in the pharmaceutical industry these days since a range of recently developed pharmaceuticals are based on this product class. Prominent examples are Vildagliptin®, Saxagliptin® or NVP-DPP-728, which are active pharmaceutical ingredients against diabetes type II and at least two of them are already successfully on the market. Important precursors of these so-called "gliptins" 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. Furthermore, the production of the latter one includes toxic precursors like oxalylchloride and phosphorylchloride. Currently, e.g. the synthesis of Vildagliptin® starts from an enantiomerically pure amino acid (here L-proline), which is transformed first into an amide derivative and then via Vilsmeier reagent into the nitrile product (process by Novartis).

A German university invented 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. The innovative reaction is also using amino acids as precursors but they are then transformed via an aldehyde intermediate into its corresponding aldoxime, which subsequently is transformed via a chemocatalytic dehydration to the nitrile target molecule.
The described technology enables a safe, fast and competitive chemical production of specific N-acyl-a-aminonitriles or N-sulfonyl-a-aminonitriles, serving as intermediates for the synthesis of, e.g., Vildagliptin®.

The university offers a license agreement as well as a technical cooperation agreement to pharmaceutical or chemical enterprises. A technical cooperation could include the implementation, repectively adaptation of this alternative technology to the existing production process of a company.
Advantages and Innovations:
Compared to the current proceedings the herewith presented invention avoids the need of toxic reagents to produce the intermediates for the synthesis of gliptins. Other competitive advantages are:
- 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
Stage of Development:
Field tested/evaluated
IPs:
Patent(s) applied for but not yet granted
CommeR Statunts Regarding IPR Status:
Patent applied for in Germany; priority year.

Partner sought

Type and Role of Partner Sought:
The university offers a license agreement as well as a technical cooperation agreement. The offer addresses in particular pharmaceutical enterprises and possibly large chemical enterprises, who produce pharmaceutical ingredients. But also small chemical enterprises, who offer these substances as part of a research tool, are potential partners.

A technical cooperation could include the implementation and adjustment of this alternative technology to the existing production process of a company.

Client

Type and Size of Client:
University
Already Engaged in Trans-National Cooperation:
Si
Languages Spoken:
English
German

Keywords

Technology Keywords:
06002001 Bioquímica / biofísica
06001015 Productos farmacéuticos / medicamentos