Four amidine NR2B-selective NMDA receptor antagonists, N-( 2-methoxy benzyl) -3-phenyl-acrylamidine, N-[diduterio(2-methoxyphenyl) methyl]-3-phenyl-acrylamidine, N-benzyl-3-phenyl-acryl amidine and N-[diduterio(phenyl)methyl]-3-phenyl-acrylamidine, all fourlabeled with carbon-14 in the 1-position, have been synthesized as part of 5-step sequence fromBa14CO3.

in view of potential biological activities of small molecule polyamides, we synthesized some novel n-(2-aminoethyl)-1-benzyl-2- (alkylthio)-1h-imidazole-5-carboxamide (7a,b), and n-(2-(1-benzyl-2-(alkylthio) -1h-imidazole- 5-carboxamido) ethyl)-1-benzyl-2- (alkylthio)-1h-imidazole-5-carboxamides (8a,b) as antitumor agents. the antitumor activity of compounds 7a,b and 8a,b was studied at concent...

The macamides are a distinct class of secondary metabolites that have so far been found only in Lepidium meyenii Walp. (Maca). Using HPLC-UV-MS/MS, the main macamides have been identified as n-benzylhexadecanamide, n-benzyl-(9Z)-octadecenamide, n-benzyl-(9Z, 12Z)-octadecadienamide, n-benzyl-(9Z, 12Z, 15Z)-octadecatrienamide and n-benzyloctadecanamide. The identities of n-benzyl-(9Z)-octadecenam...

The total synthesis of two natural phenolglycosides of the family Salicaceae, namely: populoside and 2-(β-d-glucopyranosyloxy)-5-hydroxy benzyl (3-methoxy-4-hydroxy) cinnamoate and nine not found yet in plants acyl derivatives of phenoglycosides: 2-(β-d-glucopyranosyloxy)-benzylcinnamoate, 2-(β-d-glucopyranosyloxy)-benzyl (4-hydroxy) benzoate, 2-(β-d-glucopyranosyloxy)-benzyl (3-methoxy-4-hydro...

Dehydrative reactions can be used for a wide variety of transformations including etherifications, esterifications and thioetherifications. Generally, this route is more environmentally friendly than classical methods (Williamson and Ullmann) as the only byproduct is water, whereas the use of strongly basic alkoxides or phenoxides with alkyl or aryl halides in the Williamson method produces con...

Iridium-catalyzed intramolecular [4 + 2] cycloadditions of diene-tethered alkynyl halides were investigated by using [IrCl(cod)](2) as catalyst, and dppe was found to be the most suitable phosphine ligand for the reaction. No oxidative insertion of the iridium into the carbon-halide bond was observed, and the reactions proceeded to provide the halogenated cycloadducts in good yield (75-94%). Th...

This account reviews transition metal-catalyzed C–C bond formation reactions using alkyl halides, which have rarely been used as carbon sources in conventional transition metal-catalyzed systems. In the reactions, ate complexes formed by the reaction of transition metals with a Grignard reagent play important roles as the active catalytic species. The reactions mentioned here are mechanisticall...

[reaction: see text] New air-stable PdCl(2){P(t)Bu(2)(p-R-Ph)}(2) (R = H, NMe(2), CF(3),) complexes represent simple, general, and efficient catalysts for the Suzuki-Miyaura cross-coupling reactions of aryl halides including five-membered heteroaryl halides and heteroatom-substituted six-membered heteroaryl chlorides with a diverse range of arylboronic acids. High product yields (89-99% isolate...

A highly efficient and selective synthesis of (1E)- or (1Z)-1,2-dihalo-1,4-dienes via Pd-catalyzed coupling of haloalkynes and allylic halides is described. The (1E)-1,2-dihalo-1,4-dienes were generated in good yields with excellent stereoselectivities (1E/1Z up to >98/2), while (1Z)-1,2-dihalo-1,4-dienes were produced in excellent yields and stereoselectivities (1Z/1E up to >98/2) by simply ad...