Synthesis of multi-functionalized benzofurans through the condensation of ninhydrin and phenols using SSA as a recyclable heterogeneous acid catalyst
A simple and efficient one-pot methodology has been developed for the synthesis of biologically important multi-functionalized 3-(2$$^{\prime }$$′-hydroxyaryl)-2-(2$$^{\prime }$$′-carboxyphenyl)benzofurans using silica sulfuric acid (SSA) as a heterogeneous acid catalyst in DMF medium. The significant advantages of this methodology are the use of SSA as a recyclable solid acid catalyst, operational simplicity, easy availability of the starting materials, and good yield of the products with high atom-economy.
Novel Non‐toxic and Non‐hazardous Solvent Systems for the Chemistry of Indoles: Use of a Sulfone‐containing Brønsted Acid Ionic Liquid Catalyst in Butyl Acetate
Dipolar and aprotic solvents are often required in acid‐catalyzed reactions, however, many of them are listed in solvent selection guides as not‐recommended due to their toxicity or explosivity. A catalytically functionalized ionic liquid, namely a sulfone‐containing imidazolium‐based Brønsted acid ionic liquid, was synthesized. It alleviates the detrimental effect of classical dipolar aprotic solvents because this ionic liquid integrates the function of a dipolar aprotic solvent able to stabilize carbocation intermediates and the activating effect of a strong Brønsted acid on electrophiles. The use of this tailor‐made ionic liquid was exemplified in some transformation reactions of indoles, which proceeded with high yield and selectivity using a green and an industrially acceptable solvent, butyl acetate. The recyclability of the ionic liquid catalyst was also demonstrated.
Selective histamine H3 receptor antagonists for treatment of cognitive deficiencies and other disorders of the central nervous system.
Evidence exists to implicate the monoamine histamine in the control of arousal and cognitive functions. Antagonists of H(3) receptors are postsynaptic and presynaptic modulators of neural transmission in a variety of neuronal circuits relevant to cognition. Accumulating neuroanatomical, neurochemical, pharmacological, and behavioral data support the idea that H(3) receptor antagonists may function to improve cognitive performances in disease states (e.g., Alzheimer's disease and mild cognitive impairment states). Thus, H(3) receptor antagonists have been shown to increase performance in attention and memory tests in nonhuman experiments and prevent the degradation in performances produced by scopolamine, MK-801, or age. In contrast, agonists of the H(3) receptor generally produce cognitive impairing effects in animal models. The role of H(3) receptors in these behavioral effects is substantiated by data indicating a central origin for their effects, the selectivity of some of the H(3) receptor antagonists studied, and the pharmacological modification of effects of H(3) receptor antagonists by selective H(3) receptor agonists. Data and issues that challenge the potential role for H(3) receptor antagonists in cognitive processes are also critically reviewed. H(3) receptor antagonists may also have therapeutic value in the management of obesity, pain, sleep disorders, schizophrenia, and attention deficit hyperactivity disorder.