1,4-Di-(1-Ar-o-carboran-2-yl)benzene (Ar = 3,5-bis(trifluoromethyl)phenyl (1), phenyl (2), 4-n-butylphenyl (3), 4-N,N-dimethylaniline (4)) compounds that are electronically modulated at the C1-position of o-carborane with the electron-withdrawing or -donating aryl groups were prepared and characterized. The X-ray crystal structures of 1, 3, and 4 reveal that the two aryl groups on the C1-carbor...

The direct synthesis of aryl triflones, that is, trifluoromethanesulfonyl arenes, was achieved through the trifluoromethanesulfonylation of benzynes. The trifluoromethanesulfonyl group, one of the fluorinated functional groups, is a highly electron-negative and mild lipophilic substituent. Aryl triflones have high potential in the synthesis of bioactive compounds and specialty materials. The tr...

Ultrafast photochromic molecules are being actively investigated to meet the demand for fast optical switching systems. Inspired on irreversible cyclization of 9-phenylphenalenone plant metabolites yield highly-coloured naphthoxanthenes purpose defense against pathogens, aryl-substituted phenalenones have been developed that undergo a similar but reversible reaction. The lifetime naphthoxanthen...

A method was developed for the synthesis of α-alkyl, α-aryl-bislactim ethers in good to excellent yields and high diastereoselectivities, consisting of a facile one-pot procedure in which the aryl group is introduced by means of a nucleophilic addition to benzyne and the alkyl group by alkylation of a resultant benzylic anion. Hydrolysis of the sterically less hindered adducts gave the correspo...

In the recent years there has been an increased interest in the pyridazinone ring system. Many investigations indicated that the presence of at least one aryl group, one or two electron donor atoms and/or an NH group in a special spatial arrangement is necessary for anticonvulsant activity. Many investigations indicated that the presence of at least one aryl group, one or two electron donor ato...

Inhibitors of sulfatase-2 are putative anticancer agents, but the discovery of potent small molecules targeting this enzyme has proved challenging. Based on molecular modelling, two series of sulfatase-2 inhibitors have been developed with biphenyl and biphenyl ether scaffolds judiciously substituted with sulfamate, carboxylate and other polar groups (e.g. amino). Inhibition of aryl sulfatase A...

A series of eight 3-oxapentane podand derivatives was successfully prepared based on the croton condensation reaction from 1,5-bis(aryl)-1,5-dithia-3-dioxadecane and 1,5-bis(aryl)-1,3,5-trioxadecane with bezaldehyde or acetophenone in acidic condition. These synthesized have structure acyclic crown rings inserted by polyether polythiaether chain vinyl ketone conjugated aryl group. Therefore, th...

A new method for the enantioselective reductive coupling of aryl alkenes with activated carboxylic acid derivatives via copper hydride catalysis is described. Dual catalytic cycles are proposed, with a relatively fast enantioselective hydroacylation cycle followed by a slower diastereoselective ketone reduction cycle. Symmetrical aryl carboxyclic anhydrides provide access to enantioenriched α-s...

A copper-mediated radiofluorination of aryl- and vinylboronic acids with K(18)F is described. This method exhibits high functional group tolerance and is effective for the radiofluorination of a range of electron-deficient, -neutral, and -rich aryl-, heteroaryl-, and vinylboronic acids. This method has been applied to the synthesis of [(18)F]FPEB, a PET radiotracer for quantifying metabotropic ...

A routine thioketal protecting group reacts rapidly and selectively with singlet oxygen to reveal ketone products in good (aryl 1,3-dithiolane) to excellent (aryl 1,3-oxathiolane) yields. Arylthiolanes are stable to biologically relevant reactive oxygen species and can be used as a light-activated gating mechanism for activating fluorescent sensors or small molecule prodrugs.