A mechanistic investigation of the Pd-catalyzed conversion of aryl triflates to fluorides is presented. Studies reveal that C-F reductive elimination from a LPd(II)(aryl)F complex (L = t-BuBrettPhos or RockPhos) does not occur when the aryl group is electron rich. Evidence is presented that a modified phosphine, generated in situ, serves as the actual supporting ligand during catalysis with suc...

The first general procedure for the synthesis of 5 to 7-membered 1-aryl-2-iminoazacycloalkanes is presented, by microwave-assisted ring closure of ω-arylaminonitriles promoted by polyphosphoric acid (PPA) esters. 1-Aryl-2-iminopyrrolidines were easily prepared from the acyclic precursors employing a chloroformic solution of ethyl polyphosphate (PPE). The use of trimethylsilyl polyphosphate (PPS...

The S-(5-aryl-1,3,4-oxadiazol-2-yl) O-alkyl carbonothioate (4-9) and the alkyl 2-((5-aryl-1,3,4-oxadiazol-2-yl)thio) acetate (10-15) were synthesized by interaction of 5-aryl-1,3,4-oxadiazole-2-thiones with esters chloroformic acid chloroacetic acid. yields target compounds (7-9) obtained isobutyl chloroformate 69-73%, (4-6) propyl - 74-79% 86-92%, respectively. structures confirmed IR, UV, 1H ...

4-Aryl-1,3-dihydroxy-2-naphthoates having the less accessible 1,2,3,4-tetrasubstituted naphthalene scaffold and that show photoluminescence emission from solid state as well in solutions, were selectively synthesized brominated lactol silyl ethers through 1,2-aryl-migrative ring rearrangement reaction.

The serotonin-sensitive aryl acylamidase was partially purified from monkey brain. The aryl acylamidase activity was inhibited by serotonin (Ki = 0.425 mM) and tryptamine (Ki = 3.6 mM) but not by a number of other amines. It was also inhibited by acetylcholine (Ki = 2 mM) and its analogues and homologues. The relationship of aryl acylamidase to acetylcholinesterase was examined. The ratios of s...

In this study, a class of bis-1,2-(4-aryl-2-alkyl-1H- inden-1-yl) ethane was synthesized and characterized by spectroscopic methods such as 1HNMR, 13CNMR, melting point and FTIR. bis-1,2-(4-aryl-2-alkyl-1H- inden-1-yl) ethane was synthesized by the reaction of butyl­lithium, arylindenes and dibromoethane in a facile, one-pot strategy. It’s shown that these methods have a wide scope to afford li...

The addition of aryl groups to unactivated olefins represents a direct approach to C!C bond construction. Pd-catalyzed coupling of aryl halides with alkenes, the Heck reaction, offers a viable approach to arylation. However, terminal unactivated olefins often display low reactivity in Heck reactions and can yield mixtures of styrenes and allyl arenes owing to poor regiocontrol in the b-hydride ...

Selective functionalization reactions of aromatic and heteroaromatic halides with carbon, oxygen, and nitrogen nucleophiles have attracted much attention in the last decades. In addition to typical metal-catalyzed coupling reactions, direct functionalization of aryl halides through the formation of Grignard reagents offer new ways for the efficient construction of biologically interesting carbo...

A one-pot, tandem process has been developed for the synthesis of a library of tetrazoles from aryl isothiocyanates. Condensation of aryl isothiocyanates with ammonia, and aryl amines (R-NH(2)) provided mono, 1,3-disubstituted symmetrical and unsymmetrical thioureas, which on desulfurization with molecular iodine (I(2)) led to formation of the corresponding heterocumulene (cyanamides or carbodi...

2-(Alkyl(aryl)amino)thiazol-4(5H)-ones can regioselectively be prepared from monoalkyl(aryl)thioureas and maleimides. In solution, the former heterocycles exist in a tautomeric equilibrium with 2-(alkyl(aryl)imino)thiazolidin-4-ones and the substituent on the exocyclic nitrogen atom governs the ratio of these tautomers. Isomers with the alkyl group in the endocyclic position can be obtained fro...