Dynamic kinetic asymmetric amination of branched allylic acetimidates has been applied to the synthesis of 2-alkyl-dihydrobenzoazepin-5-ones. These seven-membered-ring aza ketones are prepared in good yield with high enantiomeric excess by rhodium-catalyzed allylic substitution with 2-amino aryl aldehydes followed by intramolecular olefin hydroacylation of the resulting alkenals. This two-step ...

We herein describe the synthesis and positive modulatory activities of a small library of flavan-3-ol derivatives on alpha(1)beta(2)gamma(2L) GABA(A) receptors. Structure-activity relationships of various substituents on the A, B and C rings were evaluated in a functional electrophysiological assay. A trans configuration and a 3-acetoxy moiety are essential for activity. Substitution of the B r...

The generation of a small and representative library of 3,5,8-trisubstituted coumarins (21 compounds, 7 families, 3 groups) is described. The library was built from the corresponding propargyl vinyl ethers and three different 1,3-dicarbonyl derivatives using a one-pot coupled domino strategy. These coumarins constitute a novel chemotype defined by the presence of a chemical handle in the pyrano...

In 192 operated patients with tumors and tumorlike diseases functional results were analyzed. 162 radical sparing operations performed according to oncologic demands preservation of static-dynamic function pelvic girdle lower extremity. High efficacy those was confirmed by clinical biomechanical data. Long term showed the necessity perfect reconstructive surgery on posterior semi-ring. Elaborat...

The mol-ecule of the title compound, C(10)H(9)NO(5), is approximately planar, with the mean planes of the nitro, carboxyl and all-yloxy groups rotated by 8.1 (3), 7.9 (3) and 4.52 (18)°, respectively, from the plane of the benzene ring. Bond lengths in the aromatic ring are influenced by both electronic effects and strain induced by ortho-substitution. In the crystal structure, centrosymmetrica...

Heterocyclic compounds have paying strong attention interest. Many different derivatives have been prepared and possess various type useful pharmacological activities. A lot of work has been done on five member heterocyclic triazole ring system. Different pharmacological activities of triazole ring and its derivatives have been observed. Triazole derivatives possess a wide range of pharmacologi...

Intramolecular nucleophilic aromatic substitution (Truce–Smiles rearrangement) of the anions 2-benzyl benzanilides leads to triarylmethanes in an operationally simple manner. The reaction succeeds even without electronic activation ring that plays role electrophile SNAr reaction, being accelerated instead by preferred conformation imposed tertiary amide tether. substituent product may be remove...