Intermediates for the pharmaceutical industry
Evonik offers a broad range of intermediates for use in the pharmaceutical industry
Many of our intermediates are based on amino acids – which act as valuable precursor compounds for chiral substances – or on benzophenones. We offer extensive expertise in the manufacture and purification of derivatives of readily available L-amino acids. In addition to the amino acids above, we offer a range of non-natural amino acids and derivatives that cannot be sourced from any other major amino acid supplier. This one-of-a-kind portfolio amply demonstrates Evonik’s capabilities in the intermediates field.
Evonik has in-depth knowledge of quaternary phosphonium compounds and their derivatives – from pilot-scale production to commercial manufacturing. We also specialize in the development of high-purity stable phosphoranes in salt-free form.
We have a highly impressive track record in custom manufacturing, from small quantities of just a few kilograms to far larger scales (up to several metric tons). Our portfolio comprises the following classes of compounds:
a) Alkyltriphenylphosphonium halides (Cl, Br, I)
b) Alkyltriphenylphosphonium salts (hydroxides, acetates, phosphates)
c) Carboxyalkyltriphenylphosphonium halides
d) Carboxyalkoxytriphenylphosphonium halides
e) Stable phosphoranes (ylides) derived from c) or d)
What makes these products unique?
These products have a number of important and valuable properties. For example, they have a consistently high purity – typically between 99 and 99.5 percent – and a high isomer purity that is crucial for Wittig synthesis. Other features of these compounds include high color stability, high crystallinity and bulk density, good solubility properties, high stability against thermal and hydrolytic influences and a narrow melting range.
A host of potential applications
These properties make Evonik’s quaternary phosphonium compounds suitable for diverse applications. One of the most important uses of phosphonium compounds is as a reaction partner in organic synthesis, such as Wittig synthesis. Practical applications of this reaction include the manufacture of vitamins (A and E), the development of scents or flavorings, the synthesis of natural substances with one or more double bonds, the formation of liquid crystals or liquid crystal components and the synthesis of special plastics and polymers. Moreover, the compounds can be deployed as phase-transfer catalysts for the synthesis of various substance classes, or as catalysts in the manufacture of polymers – including polyesters, polyethers and epoxy resins.
Benzophenones are important intermediates in the field of API synthesis for Benzodiazepines, a class of controlled substances being used therapeutically as sedatives, anxiolytics, or hypnotics. Evonik Health Care offers a variety of benzophenones. As an example, Evonik produces 2-(Bromacetamido)-2,5-dichlorobenzophenone which is used as a starting material for the synthesis of important APIs like Lorazepam or Lormetazepam.
Special boronic acid esters are versatile key intermediate for synthesis of various APIs used in the field of oncology. Evonik Health Care has the competencies and assets to produce such complex intermediates at large scale with superior quality. Evonik has deep expertise in the difficult reaction conditions required to make special boronic acid esters including cryogenic cooling and handling of self-igniting reagents. Evonik also has the ability to produce small quantities for early phase development as well as scale up to multi-kilogram GMP campaigns for your commercial launch quantities.
Chiral molecules are an important part of pharmaceutical API synthesis. Chiral molecules occur in two mirror images which are non-superimposable. Evonik Health Care excels at producing chiral molecules with high optical purity often achieving enantiomeric excess (ee) values of greater than 99 percent.
L-Alanine isopropyl ester hydrochloride
L-Lysine 50 %- solution
1-Methyl-1H-pyrazole-5-boronic acid pinacol ester
L-Ornithine ethyl ester
L-Serine methyl ester HCl
D-Tryptophan methyl ester
L-Valine methyl ester
1- Methyl-1H-pyrazole- boronic acid pinacole ester