O. Schnider

Bio: O. Schnider is an academic researcher from Hoffmann-La Roche. The author has an hindex of 8, co-authored 9 publications receiving 194 citations.

Synthese von Oxy‐morphinanen

Abstract: Auf verschiedenen Wegen wurden Oxyderivate der N-Alkyl-morphinane gewonnen. Unter diesen zeichnet sich das 3-Oxy-N-methyl-morphinan durch besonders intensive und langanhaltende analgetische Wirkung aus, die auch bei oraler Verabreichung hervortritt.

Synthese von Morphinanen. (2. Mitteilung)

Abstract: Cyclohexen-(1)-yl-athylamin wird aus Cyclohexenyl-acetonitril oder Cyclohexenyl-acetamid gewonnen. Es dient als Ausgangsprodukt zur Herstellung von 1-Benzyl-, 1-(p-Methoxybenzyl)-, 1-(3′,4′-Dimethoxybenzyl)-1,2,3,4,5,6,7,8-octahydro-isochinolin.

Oxy‐morphinane. (3. Mitteilung). Optisch aktive 3‐Oxy‐morphinane

Abstract: 3-Oxy-N-alkyl-morphinane wurden in die optischen Antipoden gespalten und diese in Ather und Ester ubergefuhrt.

Synthesis of Pyridine and Dihydropyridine Derivatives by Regio- and Stereoselective Addition to N-Activated Pyridines

Abstract: Stereoselective Addition to N-Activated Pyridines James A. Bull,‡ James J. Mousseau, Guillaume Pelletier,† and Andre ́ B. Charette*,† †Department of Chemistry, Universite ́ de Montreál, P.O. Box 6128, Station Downtown, Montreál, Queb́ec, Canada H3C 3J7 ‡Department of Chemistry, Imperial College London, South Kensington, London SW7 2AZ, U.K. Department of Chemistry, Massachusetts Institute of Technology, 77 Massachusetts Avenue, Cambridge, Massachusetts 02139, USA

Asymmetric homogeneous hydrogenations at scale

Abstract: Asymmetric hydrogenations are increasingly being used to introduce stereogenic centres into products used in the life sciences industries. There are a number of potential pitfalls when moving from a laboratory reaction to a manufacturing process, not least of which is safety. Time-to-market pressure leads to short development times, which in the past could be a large barrier for the implementation of catalytic steps; now there are new ways to minimise this problem. The potential problems associated with impurities and other methods that can shut down the hydrogenation reactions are highlighted in this critical review (353 references).

The Knoevenagel Condensation

Abstract: Knoevenagel's first papers in this field were concerned with the condensation of formaldehyde with diethyl malonate and with ethyl benzoylacetate. The catalyst was ethylamine. A number of other aldehydes were reported to condense similarly with diethyl malonate, ethyl benzoylacetate, ethyl benzoylpyruvate, and acetylacetone under the influence of various primary and secondary amines. In 1896, Knoevenagel reported benzaldehyde with ethyl aceoacetate condensed at room temperature in the presence of piperdine to give a bis compound, but that when the reaction was run in a freezing mixture, the product was acetoacetate. For the purposes of this chapter, the Knoevenagel condensation is defined as the reaction between an aldehyde or ketone or any compound having an active methylene group, brought about by an organic base or ammonia and their salts. Keywords: Knoevenagel condensations; decarboxylation; malonic acid; active methylene component; stereochemical aspects; cyanoacetic acid; ketones; derivatives. caatalysts; experimental conditions

Drug specificity of pharmacological dystonia.

Abstract: Three (+)-benzomorphans that bind to sigma receptors produced dystonia in a dose-related manner when microinjected into the red nucleus of rats. Two lines of evidence suggest that these effects were related to the sigma-binding properties of the compounds. First, the behavioral potency of the (+)-benzomorphans and other active sigma compounds correlated highly with their affinities for [3H]1,3-di-o-tolylguanidine-labelled sigma receptors in the rat brain (r = .94). Second, similar intrarubral injections of non-sigma ligands were without effect: various vehicles, a structurally related (+)-opiate with no affinity for sigma receptors, and selective dopaminergic and serotonergic compounds failed to significantly alter the normal posture of rats. The only ligand in this study that binds with high affinity to sigma receptors, but failed to elicit torsional head movements was (+)-[3-(3-hydroxyphenyl)-N-(1-propyl)piperidine] [(+)-3PPP], a ligand with mixed activity at sigma and dopamine receptors. Since (+)-3PPP failed to produce an effect on its own and also failed to attenuate the dystonia produced by another sigma ligand (DTG), it may interact with a non-sigma mechanism or with a different sigma receptor type from the other compounds.