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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 and constitutes a powerful tool for the generation of valuable internal standard materials for LC-MS/MS analyses highly demanded for various life-science applications.
One-pot synthesis of human metabolites of SAR548304 by fungal peroxygenases.
The enzymatic approach revealed that the UPO of Marasmius rotula is particularly suitable for selective N-dealkylation of the drug and enabled us to prepare both human metabolites via one-pot conversion with an overall yield of 66% N,N-di-desmethyl metabolite and 49% of N-mono-des methylated compound in two separated kinetic-controlled reactions.
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 or
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 that
Preparation of labeled human drug metabolites and drug-drug interaction-probes with fungal peroxygenases.
This work shows that UPOs can be used in combination with hydrogen/deuterium exchange for an efficient one-step process for the preparation of 4'-OH-diclofenac-d6" and shows that the deuterium-labeling does not affect the kinetic parameters.
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 with
Mechanistic investigations of the liver toxicity of the free fatty acid receptor 1 agonist fasiglifam (TAK875) and its primary metabolites
The acyl glucuronide metabolites of TAK875 have been finally identified to be the dominant reason for liver toxicity.
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 drug
Malaria still a threat to life--a postmortem study.
The commonest presenting symptoms were fever with chills associated with central nervous system (CNS) complaints like altered sensorium and unconsciousness, and cerebral malaria (CM) topped the list.
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 the