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Ruthenium-catalyzed selective α,β-deuteration of bioactive amines.
A novel and convenient protocol for the catalytic hydrogen-deuterium exchange of biologically active tertiary amines utilizing the borrowing hydrogen methodology has been developed. In the presenceExpand
  • 81
H/D-exchange reactions with hydride-activated catalysts†
A safe, user friendly and efficient method to provide high deuterium incorporation into a variety of organic substrates was developed. Systematic screening of catalysts and activators revealed thatExpand
  • 21
Preparation of labeled human drug metabolites and drug-drug interaction-probes with fungal peroxygenases.
Enzymatic conversion of a drug can be an efficient alternative for the preparation of a complex metabolite compared with a multi-step chemical synthesis approach. Limitations exist for chemicalExpand
  • 14
Vanadium(II)‐ and Niobium(III)‐Induced, Diastereoselective Pinacol Coupling of Peptide Aldehydes to Give a C2‐Symmetrical HIV Protease Inhibitor
Peptide aldehydes 15 a–c are prepared without epimerization from enantiomerically pure (S)-α-amino acids (Scheme 3). Reductive pinacol homocoupling of 15 a–c, induced by vanadium complex 11 orExpand
  • 34
One-pot synthesis of human metabolites of SAR548304 by fungal peroxygenases.
Unspecific peroxygenases (UPOs, EC 1.11.2.1) have proved to be stable oxygen-transferring biocatalysts for H2O2-dependent transformation of pharmaceuticals. We have applied UPOs in a drug developmentExpand
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Dynamic Kinetic Resolution of α-Amino Acid Esters in the Presence of Aldehydes
A convenient procedure for the racemization of α-amino acid esters in the presence of catalytic amounts of salicylaldehydes is described. The combination of this racemization protocol withExpand
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Mechanistic investigations of the liver toxicity of the free fatty acid receptor 1 agonist fasiglifam (TAK875) and its primary metabolites
For fasiglifam (TAK875) and its metabolites the substance‐specific mechanisms of liver toxicity were studied. Metabolism studies were run to identify a putatively reactive acyl glucuronideExpand
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The synthesis of selected phase II metabolites – Ο-glucuronides and sulfates of drug development candidates
We have summarized methods for the preparation of phase II metabolites which have proven to be successful in our laboratory for the synthesis of selected O-glucuronides and sulfates of recent drugExpand
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A method for the enantioselective production of amino acids and amino acid derivatives using racemization catalysts
The invention beshreibt a method for the enantioselective production of amino acids or amino acid derivatives from esters thereof by reaction of mixtures of enantiomers and / or diastereomers of theExpand
  • 1
A process for preparing Diarylcycloalkylderivaten
A process for preparing a compound of general formula (I) comprising the steps according to the following scheme: wherein in the individual steps a1) a compound of formula (IX) with water (to aExpand