Several compounds have been identified that display low-efficacy, "partial substrate" activity. Here, we tested the hypothesis that the mechanism of this effect is a slower rate of induced neurotransmitter efflux than that produced by full substrates. Biogenic amine transporter release assays were carried out in rat brain synaptosomes and followed published procedures. [(3)H]1-methyl-4-phenylpy...

The synthesis and the evaluation as organocatalysts of new chiral guanidines derived from benzimidazoles in the enantioselective α-amination of 1,3-dicarbonyl compounds using di-t-butylazodicarboxylate as aminating agent is herein disclosed. The catalysts are readily synthesized through the reaction of 2-chlorobezimidazole and a chiral amine in moderate-to-good yields. Among all of them, those ...

An efficient and convenient synthesis of novel tetrahydrobenzo[c]acridin-8(7H)-one derivatives is described using the electrogenerated anion of acetonitriles as the base in the presence of tetrabutylammonium fluoride as an effective supporting electrolyte in a one-pot, three-component condensation of aromatic aldehyde, dimedone and 1-naphthyl amine. The reaction is carried out in an undivided c...

A new method for preparing naphthyl amines from 1,5 unsaturated dicarbonyl precursors is described; the utility of this new method was proven in the syntheses of several natural products, all containing the benzo[c]phenanthridine core and enabled by a radical promoted cyclisation of the naphthyl amine products formed in the key cyclisation.

The reaction of 1-naphthyl-methyl-amine and hydro-chloric acid in a 1:1 molar ratio resulted in the formation of the 1:1 proton-transfer compound, C(11)H(12)N(+)·Cl(-). In the crystal, the ions are linked by N-H⋯Cl hydrogen bonds into a sheet pattern in the ab plane such that each Cl(-) ion is bonded to three NH groups from the naphthylmethylammonium ion.

The title compound, C(23)H(19)N, was obtained unexpectedly from the reaction of [Eu(nta)(3)(PzPy)] {Hnta = 1-(2-naphtho-yl)-3,3,3-trifluoro-acetone and PzPy = 2-[3(5)-pyrazol-yl]pyridine} with 1-naphthyl-methyl-amine. The 1- and 2-naphthyl groups are essentially planar [r.m.s. deviations of 0.007 and 0.011 Å, respectively] and subtend angles of 38.69 (11) and 16.50 (11)°, respectively, with the...

Previous investigations have shown that the major cellobiohydrolase of Phanerochaete chrysosporium, Cel7D (CBH 58), can be used to separate the enantiomers of a number of drugs, including adrenergic beta blockers such as propranolol. The structural basis of this enantioselectivity is explored here. A 1.5 A X-ray structure of the catalytic domain of Cel7D in complex with (R)-propranolol showed t...

The synthesis, protonation behavior, and Cu2+ and Zn2+ coordination chemistry of the novel bibrachial aza lariat ether (naphthalen-1-ylmethyl)[2-(20-[2-[(naphthalen-1-ylmethyl)amino]ethyl]-3,6,9,17,20,23,29,30-octaazatricyclo[23.3.1.1*11,15*]triaconta-1(29),11(30),12,14,25,27-hexaen-6-yl)ethyl]amine (L) are discussed. The macrocycle, which has two aminoethyl naphthyl moieties symmetrically appe...

Three series of P-chiral diphosphines based on ferrocene (1a-f, 2a-c) and biferrocenyl skeletons (3a-c), including novel ligands 1f and 3c, were employed in palladium-catalyzed allylic substitution reactions. Steric effects imposed by the phosphine residues were studied using C2-symmetrical donors 1 (1 = 1,1'-bis(arylphenylphosphino)ferrocene with aryl groups a = 1-naphthyl, b = 2-naphthyl, c =...