Whereas arginine vasopressin binds to its receptor subtypes V(1)R and V(2)R with equal affinity of approximately 2 nM, nonpeptide antagonists interact differently with vasopressin receptor subtypes. The V(2)R antagonist binding site was mapped by site-directed mutagenesis at six selected amino acid positions, K100D, A110W, M120V, L175Y, R202S, and F307I, predicted to be involved in antagonist b...

In the title compound, C(18)H(21)N(3)O(2)·H(2)O, the fused-ring system is approximately planar [maximum atomic deviation = 0.028 (3) Å]; the morpholine ring displays a chair conformation. The crystal packing is stabilized by classical inter-molecular O-H⋯O and O-H⋯N hydrogen bonds and weak C-H⋯O hydrogen bonds between the organic mol-ecules and the water mol-ecules.

A review of the recent literature is given focusing on synthetic approaches to 1,2,3,4-tetrahydroquinolines, 2,3-dihydro-4(1H)-quinolinones and 4(1H)-quinolinones using domino reactions. These syntheses involve: (1) reduction or oxidation followed by cyclization; (2) SNAr-terminated sequences; (3) acid-catalyzed ring closures or rearrangements; (4) high temperature cyclizations and (5) metal-pr...

The seven-membered fused-ring in the title compound, C(10)H(10)N(2)O·H(2)O, adopts a boat conformation (with the two phenyl-ene C atoms representing the stern and the methyl-ene C atom the prow). In the crystal, two benzodiazepinone mol-ecules are linked about a center of inversion by diazepine-carbonyl N-H⋯O hydrogen bonds. The dimers are further linked by water-diazepine O-H⋯N hydrogen bonds,...

In the title compound, C(28)H(30)N(2)O(2), the cyclo-hexene ring system adopts a sofa conformation. The crystal structure is stabilized by C-H⋯O inter-actions between methyl H atoms of the ethyl substituents and the O atoms of carbonyl groups of adjacent mol-ecules, and by an inter-molecular carbon-yl-carbonyl inter-actions [3.207 (2) Å].

The title compound, C(9)H(11)NO(3), was prepared by an Aldol reaction of 2,3-dihydro-1H-pyrrolizin-1-one with formaldehyde. The asymmetric unit contains six mol-ecules. The pyrrolizine ring system in each mol-ecule is planar, the maximum atomic deviation being 0.066 (2) Å. In the crystal structure, mol-ecules are liked together by an extensive O-H⋯O hydrogen-bonding network.