In methanol-aqueous solutions, three novel structure-directing agents (SDAs) were generated in situ and presented. These in situ reactions feature N-methylation transformations between CH3OH solvent and organic cyclic aliphatic and aromatic amines, i.e. 2-methylpiperazine, 1,4-diazabicyclo[2,2,2]octane (dabco) and 3-(aminomethyl)pyridine. Distinct from conventional Eschweiler-Clarke methylation...

Four types of carbons (activated carbon, Maxsorb superactivated carbon, mesoporous templated carbon CMK-3, and graphene) were investigated as selective sorbents for adsorption of thiophene from its solution in n-octane. Graphene showed clearly the highest sulfur capacity. The relative sulfur capacities correlated well with the relative heats of adsorption. The carbene-type zigzag edge sites and...

One important access to monodisperse (functionalized) oligoPPEs is based on the orthogonality of the alkyne protecting groups triisopropylsilyl and hydroxymethyl (HOM) and on the polar tagging with the hydroxymethyl moiety for an easy chromatographic separation of the products. This paper provides an update of this synthetic route. For the deprotection of HOM protected alkynes, γ-MnO₂ proved to...

Asymmetric rotators with a 1,4-bis(ethynyl)bicyclo[2.2.2]octane (BCO) core are needed for engineering crystalline arrays of functional molecular rotors. Their synthesis uses carbinol, 2-methyl-3-butyn-2-ol, as a protecting group because of its polar character and its ability to sustain orthogonal functionalization with the further advantage of being readily removed. The synthesis in good yields...

The reaction of 1,5-dibenzyl-3-propargyl-1,5-benzodiazepine-2,4-dione with 1-azido-n-octane in the presence of catalysts leads to the formation of the title compound, C(34)H(39)N(5)O(2), which features a phenyl-ene ring fused with a seven-membered diazepinyl ring. The latter ring adopts a boat conformation with the octyltriazolylmethyl-bearing C atom as the prow and the fused-ring C atoms as th...

[reaction: see text]Cyclization of the optically active ketone N,N-dialkyl aminals A affords the diastereomer B as the major product with diastereoselectivities ranging from nearly 1:1 to essentially 100:0 depending on the cyclization studied.

We report structure-activity studies of a large number of dialkyl imidazoles as inhibitors of Trypanosoma cruzi lanosterol-14R-demethylase (L14DM). The compounds have a simple structure compared to posaconazole, another L14DM inhibitor that is an anti-Chagas drug candidate. Several compounds display potency for killing T. cruzi amastigotes in vitro with values of EC50 in the 0.4-10 nM range. Tw...

We report structure-activity studies of a large number of dialkyl imidazoles as inhibitors of Trypanosoma cruzi lanosterol-14alpha-demethylase (L14DM). The compounds have a simple structure compared to posaconazole, another L14DM inhibitor that is an anti-Chagas drug candidate. Several compounds display potency for killing T. cruzi amastigotes in vitro with values of EC(50) in the 0.4-10 nM ran...

Serine esterases are inhibited by dialkyl fluorinated aminophosphonate (FAP) compounds of general formula, (RO)2P(O)C(CF3)2NHS(O)2C6H5, where R = alkyl. It has been hypothesized that the active site serine of the esterase covalently attaches to the phosphoryl moiety of the FAP compound, resulting in formation of a dialkyl phosphate adduct that can age by net loss of an R-group. However, this me...

The Kinetic studies were made of the reactions between triphenylphosphine, dialkyl acetylenedicarboxylates in the presence of NH-acid, such as harman. To determine the kinetic parameters of the reactions, they were monitored by UV spectrophotometery. The second order fits were automatically drawn and the values of the second order rate constant (k2) were calculated using standard equations with...