An alternative strategy for the synthesis of 1-aryl- and 1-alkyl-2-methylsulfanyl-4-(4-fluorophenyl)-5-(pyridin-4-yl)imidazoles as potential p38α mitogen-activated protein kinase inhibitors is reported. The regioselective N-substitution of the imidazole ring was achieved by treatment of α-aminoketones with different aryl or alkyl isothiocyanates. In contrast to previously published synthesis ro...

Intermolecular photocatalytic hydroaminoalkylation (HAA) of alkenes have emerged as a powerful method for the construction alkyl amines. Although there are some studies aiming at stereoselective HAA reactions, limited to electrophilic alkenes. Herein, we report highly regio-, diastereo-, and enantioselective electron-rich dienol ethers ?-amino radicals derived from acids using unified photoredo...

Pieces of the digestive gland of the starfish, Asterias forbesi, were incubated in vitro with various radioactive lipid precursors in order to follow the biosynthesis of the alkyl and alkenyl glycerol ethers. Acetate-1-14C was incorporated readily into alkyl glycerol ethers of both neutral lipid and phospholipid fractions, but very poorly into the alkenyl glycerol ethers. Stearic acid-l-14C and...

3-Alkyl(Aryl)-4-amino-4,5-dihydro-1H-1,2,4-triazol-5-ones (2) reacted with 2-furoyl chloride and thiophene-2-carbonyl chloride to afford the corresponding 3- alkyl(aryl)-4-(2-furoylamino)-4,5-dihydro-1H-1,2,4-triazol-5-ones (3) and 3-alkyl(aryl)- 4-(2-thienylcarbonylamino)-4,5-dihydro-1H-1,2,4-triazol-5-ones (4), respectively. The new compounds synthesized were characterized by using IR, 1H-NMR...

Antimitotic natural products that bind to cellular microtubules can be used as anticancer agents, and we are studying the cellular mechanisms of these compounds.1 The fungal metabolite phomopsin A is a key structure in these studies, and we are currently pursuing its synthesis.2 Our retrosynthetic analysis of phomopsin A targeted the chiral tertiary alkyl-aryl ether as a key disconnection withi...

A mild method for the regioselective synthesis of propargyl ethers by the coupling of propargyl alcohols with a range of other alcohols is described. The method employs an air- and moisture-tolerant rhenium-oxo complex ((dppm)ReOCl3) as a catalyst for the formation of sp3-carbon-oxygen bonds without the need for prior activation of the propargyl alcohol or deprotonation of the alcohol nucleophi...

In contrast to the structurally and configurationally stable alkyl- or aryl-substituted cyclopropyl radical cations, cyclopropyl silyl ethers undergo spontaneous ring opening upon oxidation whereby the endocyclic C-C(O-TMS) bond is cleaved with remarkable selectivity. DFT calculations on 1-trimethylsilyloxybicyclo[4.1.0]heptane show that this selectivity arises from the topology of the potentia...

INTRODUCTION .......................................................................................................................................................216 PROBLEM POLLUTANTS AND ETHER SCISSION..........................................................................................217 Agrochemicals........................................................................................

A Lewis-acid promoted one-carbon homologation of an aspartic acid semialdehyde with trimethylsilyldiazomethane has led to the efficient synthesis of two silicon-containing a-amino acids. The use of trimethylaluminium or catalytic tin(II) chloride gave novel 4-oxo-5-trimethylsilanyl derived amino acids in yields of 71e88%. An investigation into the reactivity of these highly functional a-amino a...