A selection of aromatic amines has been shown to react with pentyl nitrite in the presence of bromoform to give the corresponding aryl bromides in acceptable yield. Corresponding reactions with bromotrichloromethane, chloroform, and carbon tetrachloride have been proved to be synthetically less useful.THE use of alkyl nitrites as h situ diazotising agents has received attention in connection with the formation of benzyne from anthranilic acid,l the reduction of aromatic amines in the presence of dimethylformamide,2 and aromatic arylation using aromatic acylamines and a m i n e ~. ~. ~ That the last reaction proceeds by a homolytic route has now been confirmed by the observation
The current review describes the recent progress in the
chemistry
and biology of the benzhydryl amines where the central carbon atom
is directly attached to the nitrogen atom of one ring and which have
published in the last five years (2015–2019). Both metal and
metal-free racemic and asymmetric synthetic approaches along with
their activities as anti-leishmanial, antiviral, antibacterial, and
anti-aromatase and other miscellaneous properties are discussed.
An expeditious, cost-effective synthetic methodology for a wide range of nitrogen-containing unsymmetrical trisubstituted methanes (TRSMs) is reported. The synthesis involves base-mediated 1,6-conjugate addition of heterocyclic amines and amides to substituted para-quinone methides, giving the unsymmetrical TRSMs in moderate to very good yields (up to 83%) in one pot. The low cost, mild temperature, high atom economy and yields, easy scale-up and broad substrate scope are some of the salient features of this protocol. Further, the methodology could be extended for the synthesis of meclizine-, hydroxyzine- and cetirizine-like molecules. The structure of one such compound, 2,6-di-tert-butyl-4-((4-chlorophenyl)(4-methylpiperazin-1-yl)methyl)phenol, was determined by single crystal X-ray analysis.
There has recently been an increased interest in active pharmaceutical agents and various other molecules that contain the 1, 1‐diaryl stereocenter. This has led to the development of novel synthetic strategies to access molecules having this structural moiety. The current Review describes the variety of synthetic methodologies available for the enantioselective synthesis of 1, 1‐diarylethanes, triarylmethanes and related molecules with a 1, 1‐diaryl stereogenic center that were reported since 1995. The prime focus of the Review is on the formation of the 1, 1‐diarylmethine stereocenter either through the use of various enantioselective processes using chiral catalysts (the asymmetric catalytic approach) or through the use of chiral substrates and achiral catalysts. Resolution of racemic substrates is also required for the synthesis of this chiral molecule, but this approach is not covered in this Review. Moreover, comparative discussions on the future aspects of the synthesis of these molecules with a short comparison of the different available routes and possible areas of development are also presented.
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