Intramolecular carbolithiation of N-allyl-ynamides: An efficient entry to 1,4-dihydropyridines and pyridines - Application to a formal synthesis of sarizotan
We have developed a general synthesis of polysubstituted 1,4-dihydropyridines and pyridines based on a highly regioselective lithiation/6-endo-dig intramolecular carbolithiation from readily available N-allyl-ynamides. This reaction, which has been successfully applied to the formal synthesis of the anti-dyskinesia agent sarizotan, further extends the use of ynamides in organic synthesis and further demonstrates the synthetic efficiency of carbometallation reactions.
Heterocyclic aminoalkyl pyridine derivatives as psychopharmaceuticals
The invention relates to heterocyclic aminoalkylpyridine derivatives of the formula I where R1 is the radical of a heterocycle having 1 to 3 ring structures, where each ring structure is saturated, unsaturated or aromatic and optionally fused t
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(2008/06/13)
Method for producing 5-aryl nicotinaldehydes
The invention relates to a process for the preparation of 5-arylnicotinaldehydes by reduction of the corresponding 5-arylnicotinic acids by catalytic hydrogenation in the presence of carboxylic anhydrides in which the catalyst used is a palladium/ligand complex, characterized in that the molar ratio between palladium and ligand is from 1:5 to 1:15 in the case of monodentate ligands and from 1:2.5 to 1:7.5 in the case of bidentate ligands.
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(2008/06/13)
Piperazine and piperidine compounds
A group of new piperazine and piperidine compounds having interesting advantageous pharmacological properties and have the formula (a) wherein A represents a heterocyclic group having 5-7 ring atoms wherein 1-3 heteroatoms selected from the group O, N and
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(2008/06/13)
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