The
endeavor of mastering “Nature-like Multicatalysis”
in vitro has inspired chemists to develop catalytic systems comprising
a variable number of catalysts in one-pot. Having been pioneered in
the primitive stages (particularly unary and binary catalysis), the
field has witnessed the inception of “Ternary Catalysis”
described as the concept of harnessing an ensemble effect of three
discrete catalysts in one-pot. Although the concept is nascent, it
has already demonstrated its invaluable importance in terms of producing
novel reactivity, prodigious selectivity, and efficiency. As evident
from the presented documentation, the number of pertinent reports
utilizing ternary catalysis has drastically increased in the past
few years; however, these reports remain scattered in the literature.
The conceptualization and unambiguous catalyst-dependent classification
presented herein provides an imperative unified approach to assemble
and categorize all such reports which have remained missing by far.
Special emphasis has been given to mechanistic analysis clearly disclosing
the beauty of ternary catalysis. For the better understanding of the
concept, a succinct description of challenges and problems associated
in the development of a ternary catalytic system has been presented.
In addition, the Review briefly discusses some of the unsolved problems
and possible developments in this field.
Reported
herein is the gold-catalyzed 1,2-aminoarylation of alkenes
that engages external amine as a coupling partner. Careful optimization
studies revealed a significant role of the concentration of base to
achieve highly chemoselective access to the aminoarylation products
over potential C–N cross-coupled products. Overcoming all the
limitations, the current strategy provided straightforward access
to the medicinally relevant 3-aminochroman, 2-aminotetrahydronaphthalene,
and 2-aminoindane derivatives.
Indoxacarb residues were estimated by employing standardized QuEChERS technique in cabbage following three applications of Avant(R) 14.8 EC @ 52.2 and 104.4 g a.i. ha(-1). The average recoveries of indoxacarb on cabbage for fortification levels of 0.01, 0.05 and 0.1 mg kg(-1) were observed to be 83.93, 89.86 and 95.40%, respectively, with relative standard deviation of 1.21, 1.53 and 2.23. The method was also validated with respect to parameters of linearity, precision and limit of quantification (LOQ). The LOQ for cabbage was found to be 0.01 mg kg(-1). The average initial deposits of indoxacarb on cabbage were observed to be 0.18 and 0.39 mg kg(-1), respectively, at single and double the application rate. These indoxacarb residues dissipated below its LOQ of 0.01 mg kg(-1)after 7 and 10 days, respectively, at single and double dosages. Half-life of indoxacarb was observed to be 2.88 and 1.92 days, respectively, at recommended and double the recommended dosages.
6-Endo-dig-cyclization is an efficient method for the synthesis of 1,2-dihydroisoquinolines. We have synthesized few 1,2-dihydroisoquinolines having different functionality at the C-1, C-3, C-7, and N-2 positions for evaluation against HIV-1 integrase (HIV1-IN) inhibitory activity. A direct nitro-Mannich condensation of o-alkynylaldimines and dual activation of o-alkynyl aldehydes by inexpensive cobalt chloride yielded desired compounds. Out of 24 compounds, 4m and 6c came out as potent integrase inhibitors in in vitro strand transfer (ST) assay, with IC 50 value of 0.7 and 0.8 μM, respectively. Molecular docking of these compounds in integrase revealed strong interaction between metal and ligands, which stabilizes the enzyme−inhibitor complex. The ten most active compounds were subjected to antiviral assay. Out of those, 6c reduced the level of p24 viral antigen by 91%, which is comparable to RAL in antiviral assay. Interestingly, these compounds showed similar ST inhibitory activity in G140S mutant, suggesting they can act against resistant strains.
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