DexLeChem’s first patent was granted in the US: process for the reduction of nitro derivatives to amines

The U.S. patent office has recently granted DexLeChem the patent US 9284258 B2 in its full scope. The European patent office has already communicated its intention to grant the patent as well.
DexLeChem is now looking for partners and investors to accelerate its commercialization.

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The invention “process for the reduction of nitro derivatives to amines” relates to a complete new production pathway based on the use of trichlorosilane (metal-free, very cost-efficient reducing agent[1]) and an organic base, which is useful in the synthesis of various classes of compounds of interest in the pharmaceutical, fragrances industries, and fine chemicals in general.

“That we have obtained the patent protection for all claims ensures us the broadest possible applicability for all kinds of products. This is very unusual and it clearly shows the degree of novelty and inventive ingenuity that this process possesses. With this patent protection, we are now able to secure complete new competitive advantages for our customers.” says DexLeChem CEO Sonja Jost enthusiastically."

The well-known Italian chemical manufacturer ZaCh Systems S.p.A. has acquired a first license of the invention.

For further information or if you are interested to assist us in the commercialization, please contact Mr. Martin Rahmel.

Background of the invention:

The need for a reliable methodology to insert amino groups without harming the remaining molecule structure is of big industrial importance, however, it is technically challenging.

State-of-the-art processes involve the use of catalysts like Palladium or Platinum on charcoal. As often as these methods are applied in industry as many problems occur, especially when it comes to complex drugs: other parts of the active pharmaceutical ingredients (API) are attacked and alter the needed molecule structure in an undesirable way which leads to a significant increase of the manufacturing costs; but also metal residues from the catalysts in the product can cause problems and hinder the drug approval process.

Chemical reduction methods on the other hand which in general yield higher product qualities are nowadays only very seldom applied in industry because of problems with environmentally safe waste disposals.[2]

So far, there has been no solution for most of the aforementioned problems.

Our patent now enables a complete new pathway that possesses certain advantages against the former state-of-the-art:

  • it does not attack other parts of the compounds (which is described as a high chemoselectivity)
  • the work-up is very easy and it enables an environmentally safe waste disposal as the totally non-toxic waste can be discharged into aqueous wastewater
  • there are no risks of contamination of the product by metals
  • while broadening the range of alternative synthesis routes, blocking patents can be bypassed
  • no high pressure equipment is needed
  • the chirality of drugs which is of high importance for the pharmacological effect of the drugs is not affected as it respects the stereochemical integrity of the stereogenic elements of the molecule

[1] Trichlorosilane is a bulk product in the semiconductor industry

[2] Ullmann's Encyclopedia of Industrial Chemistry, Verlag Chemie, Weinheim, New York: vol. A2 (2012), pp. 647-698; vol. A2 (2012), pp. 699-718

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