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Método eficiente de síntesis de compuestos de Biginelli con efectos farmacológicos valiosos

Resumen

Tipo:
Oferta Tecnológica
Referencia:
TOES20160905001
Publicado:
09/09/2016
Caducidad:
09/09/2017
Resumen:
Un equipo de investigación en química de una universidad española ha desarrollado un nuevo método de síntesis enantioselectiva de dihidropirimidinonas (DHPM o compuestos de Biginelli) capaz de separar y obtener el enantiómero con la actividad biológica deseada mediante un método "one-pot" de bajo coste. La universidad busca fabricantes de productos químicos en el sector farmacéutico para establecer acuerdos de licencia y explotar la tecnología.

Details

Tittle:
An efficient method for the synthesis of Biginelli´s compounds with valuable pharmacological effects.
Summary:
A chemistry research group from a Spanish university has developed a new method for the enantioselective synthesis of Dihydropyrimidinones (DHPMs or Biginelli products) which is able to separate and obtain the enantiomer with the desired biological activity through a "one-pot" and cost saving method. A licensing agreement for the exploitation of the technology is being offered to chemical products manufacturers in the pharmaceutical sector.
Description:
Dihydropyrimidinones (DHPMs or Biginelli products) are a family of compounds with a wide range of biological activity. Many of them present pharmacological activity in very different health disorders such as arrhythmia, urinary incontinence, depression or sleep disorders, as well as acting as antihypertensive agents, calcium channel modulators, melanin concentrating hormone receptor (MCHR1-R) antagonists or anticancer agents among others.

In many cases, the biological or pharmacological activity of one enantiomer is different from that of the other enantiomer and therefore it is important to provide synthetic processes which are enantioselective and result in preferentially or exclusively only one of the two enantiomers. The most common method to obtain the racemic mixture of DHPMs is the three-component reaction, named after Pietro Biginelli, but this method is a non-enantioselective preparation process. Other direct and enantioselective methods make use of metals and are therefore less environmentally friendly, whereas others need of harsh or extreme conditions or feature a poor atom economy. It is therefore widely recognized the unmet need for new efficient methodologies for the synthesis of enantiomerically pure DHPMs.

This research group with wide expertise and knowledge in the study of chemical reactions has developed a new "one pot" scalable process to obtain enantiomerically enriched DHPMs, in high yield and high enantiomeric purity and environmentally efficient, since the catalyst used is non-metallic and it can be recovered and reused.

Companies from all countries engaged in the research, development and synthesis of organic chemical products in the pharmaceutical sector to carry out a licensing agreement for the technology described are sought.
Advantages and Innovations:
· "One-pot" methodology. There is no need to isolate intermediate compounds; all reactions may be carried out without the need of any intermediate separation step.

· Scalable. The method is scalable up to 2mmol scale (just about 0.5gr).

· High chemical yield. The method has been successfully applied to more than 20 examples.

· High enantiomeric purity. One DHPM enantiomer is obtained with an enantiomeric excess greater than 95%.

· Atom economic. The method not only provides a high yield of the desired final product but also provides a high selectivity, minimizing the existence of by-products.

· Environmental efficiency. The catalyst can be easily recycled, i.e. recovered and reused with no significant loss of capacities; almost the same results in terms of chemical yield and enantioselectivity have been obtained with the recovered catalyst.
Stage of Development:
Available for demonstration
IPs:
Patent(s) applied for but not yet granted
CommeR Statunts Regarding IPR Status:
A European Patent application has been recently submitted (June, 2016) to protect the method, having the possibility to extend such protection internationally via PCT.

Partner sought

Type and Role of Partner Sought:
This technology is aimed at small, medium and large companies dedicated to product development of organic chemistry for the pharmaceutical industry through a license agreement.

Client

Type and Size of Client:
University
Already Engaged in Trans-National Cooperation:
No
Languages Spoken:
English
Spanish

Keywords

Technology Keywords:
06001015 Productos farmacéuticos / medicamentos
05001004 Química orgánica