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Your search keyword '"Jacques Cercus"' showing total 2 results
Start Over Author "Jacques Cercus" Publisher elsevier bv
2 results on '"Jacques Cercus"'

1. Synthesis of new N-aryl oxindoles as intermediates for pharmacologically active compounds

Author

Gottfried Sedelmeier, Xu David, Thomas Allmendinger, Olivier Loiseleur, Murat Acemoglu, Calienni John Vincent, and Jacques Cercus

Subjects
chemistry.chemical_compound, chemistry, Aryl, Organic Chemistry, Drug Discovery, Condensation, Organic chemistry, Dehydrogenation, Oxindole, General Medicine, Smiles rearrangement, Biochemistry, Combinatorial chemistry
Abstract

Various new N-aryl oxindoles were synthesized as intermediates for the preparation of pharmacologically active 2-(N-arylamino)-phenylacetic acids. Two novel approaches were explored for the construction of diarylamine and N-aryl oxindole core structures, in addition to Buchwald-arylamination and Smiles rearrangement. Condensation of anilines with 2-oxo-cyclohexylidene-acetic acid derivatives and subsequent dehydrogenation is a new and viable method for the preparation of N-aryl oxindoles.

Published
2004
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2. The development of a practical synthesis of the potent and selective somatostatin sst3 receptor antagonist [4-(3,4-difluoro-phenyl)-piperazine-1-yl]-{(4S,4aS,8aR)-2[(S)-3-(6-methoxy-pyridin-3-yl)-2-methyl-propyl]-decahydroisoquinoline-4-yl}-methanone (NVP-ACQ090)

Author

Markus Bänziger, Hans Hirt, Christophe Malan, Kurt Laumen, Troxler Thomas J, Felix Spindler, Jacques Cercus, and Fritz Struber

Subjects
Stereochemistry, medicine.drug_class, Organic Chemistry, Receptor antagonist, Catalysis, Inorganic Chemistry, chemistry.chemical_compound, Piperazine, Somatostatin, chemistry, Reagent, NVP ACQ090, Side chain, medicine, Physical and Theoretical Chemistry, Derivative (chemistry), Overall efficiency
Abstract

The decahydroisoquinoline derivative NVP-ACQ090 is a potent and selective antagonist at the somatostatin sst3 receptor. The original research synthesis of NVP-ACQ090 comprises a main chain of nine linear steps and two side chains of three and steps, respectively. This synthesis is highly convergent, but very complex and expensive, and involves several reagents that are not acceptable for a large scale synthesis. In chemical development, all the unacceptables could be replaced, and the overall efficiency of the synthesis was much improved.

Published
2003
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