Universidad de Alicante

Procedure for the preparation of polysubstituted pyrrolidines as inhibitors of the hepatitis C virus

Posted by Universidad de AlicanteResponsive · Patents for licensing · Spain

Summary of the technology

The research group has developed a highly enantioselective process catalysed by small amounts of a chiral complex formed by a silver(I) salt and a chiral phosphoramidite. This method allows the preparation of enantioenriched polysubstituted proline derivatives after a three-step sequence. These prolines are widely used for multiple purposes, but the most important activity is based on the high efficiency against the hepatitis C virus. The administration of these drugs in mammalians is beneficial because the risks of the multiple side effects are reduced and the required dose is very small, unlike the mixture of the pharmaceuticals employed in the current therapy. This research group asks for companies ready to acquire this methodology for a future exploitation.

Innovation features:

At this moment, this methodology is the unique dealing with the production of these antiviral agents in an highly enantioselective manner. This enantioselective synthesis is very reliable, reproducible and allows to react very bulky starting materials giving high chemical yields. This method is a clear example of the atom economy.

Description of the technology

Highly enantioselective process catalysed by small amounts of a chiral complex formed by a silver(I) salt and a chiral phosphoramidite. This method allows the preparation of enantioenriched Polysubstituted proline derivatives after a three-step sequence. These prolines are widely used for multiple purposes, but the most important activity is based on the high efficiency against the hepatitis C virus. The administration of these drugs in mammalians is beneficial because the risks of the multiple side effects are reduced and the required dose is very small, unlike the mixture of the pharmaceuticals employed in the current therapy. This research group asks for companies ready to acquire this methodology for a future exploitation.

Specifications

Main advantages of its use

  • The processes are highly enantioselectives. The final antiviral agents are obtained with very good ee’s.
  • The chemical yields are very good, and the purity of the compounds is very high.
  • The procedure is efficient and reproducible

Applications

  • PHARMACEUTICAL COMPANIES: they represent a very promising therapy against the proliferation and development of the virus responsible of the hepatitis C. Their efficiency and biological potential has been demonstrated in infected mice IC50= 0.3-0.5 μM, (even lower according to the new structures published in the literature).

Related keywords

  • Biochemistry / Biophysics Technology
  • Virus, Virology / Antibiotics / Bacteriology
  • Medical Research
  • Laboratory equipment
  • pyrrolidines
  • hepatitis C

About Universidad de Alicante

Research & Technology Organization from Spain

As one of the largest universities of Spain, Universidad de Alicante has a rich history of innovation. Our main objective is to transfer the technology that our research teams are developing to the industries and companies which are able to take profit from them. R & D & Innovation results and know-how are offered in the domains of Chemistry, Materials, Environment, IT, Building and other applied subjects.

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