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Drug metabolites

Drug metabolites - Glucuronide sulfate and acetyl formation: The times when polar metabolites could be dismissed as products with little interest are now over. Phase 2 metabolites play a crucial role in the body's process of detoxifying and eliminating harmful substances, including drugs, toxins, and endogenous compounds like hormones. This process, known as Phase 2 metabolism or conjugation, involves the addition of a water-soluble group to a molecule, making it easier for the body to excrete it via urine or bile. Our know-how allows us to the preparation of metabolites kept free form their API’s by multistep synthesis, hemi-synthesis or by direct modification of the parent drug. We have also a great experience in the synthesis of hydroxylated and glucuroconjugated metabolites. As examples, some phase 2 conjugate metabolites.

Glucuronidation of Phloroglucinol

Phloroglucinol glucuronide is a metabolite of phloroglucinol that plays a role in its elimination from the body and may have its own distinct properties compared to phloroglucinol itself.

glucuronide metabolite
 

Conjugate sulfate of resveratrol

Resveratrol is a polyphenolic compound found in various plants. The sulfate conjugates of resveratrol are important metabolites in the body’s process of eliminating the compound.

sulfate metabolite

Glycoside metabolite of Dicamba

Xenobiotics containing carboxylic acid groups are often readily metabolized to acyl glucuronides. We are specialized  in producing acyl glucuronides.

acyl glucuronide

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Drug metabolites - hydroxylation desmethylation and ketome formation: The use of metabolites leads to the real and good response expected compared to the use of other standards. Our know-how allows us to the preparation of metabolites kept free form their API’s by multistep synthesis, hemi-synthesis or by direct modification of the parent drug. We have also a great experience in the synthesis of hydroxylated and glucuroconjugated metabolites. As examples, some phase 1 metabolites.

Omeprazole hydroxylation

5-hydroxyomeprazole was obtained in 10 steps compared to the literature (21 steps). It's the main metabolite of Omeprazole

5-Hydroxy Omeprazole main metabolite
 

O-Desmethylation of Pimobendan

Synthesized metabolites are kept free of active ingredients (API's) by direct or multistep synthesis modification of the parent drug.

demethlpimobendan

N-Desmethylation of Mifepristone

Many antidepressant and antipsychotic drugs are tertiary amines, the alkyl groups are removed from the amino group by the process of oxidation. 

demethylmifepriston

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