Tetrahydroquinoline is one of the most important simple nitrogen heterocycles, being widespread in nature and present in a broad variety of pharmacologically active compounds. This Review summarizes ...the progress achieved in the chemistry of tetrahydroquinolines, with emphasis on their synthesis, during the period from mid-2010 to early 2018.
Pyrrole is one of the most important one-ring heterocycles. The ready availability of suitably substituted and functionalized pyrrole derivatives is essential for the progress of many branches of ...science, including biology and materials science. Access to this key heterocycle by multicomponent routes is particularly attractive in terms of synthetic efficiency, and also from the environmental point of view. We update here our previous review on this topic by describing the progress made in this area in the period between mid-2009 and the end of 2013.
Multicomponent mechanochemical synthesis Leonardi, Marco; Villacampa, Mercedes; Menéndez, J. Carlos
Chemical science (Cambridge),
2018, Letnik:
9, Številka:
8
Journal Article
Recenzirano
Odprti dostop
Historically, the use of mechanochemical methods in synthesis has been almost negligible, but their perception by the synthetic community has changed in recent years and they are on their way to ...becoming mainstream. However, the hybridization of mechanochemical synthesis with methodologies designed to increase synthetic efficiency by allowing the generation of several bonds in a single operation has taken off only recently, but it already constitutes a very promising approach to sustainable chemistry. In this context, we provide in this Perspective a critical summary and discussion of the main known synthetic methods based on mechanochemical multicomponent reactions.
Multicomponent reactions promoted by mechanical energy are critically reviewed.
The use of cerium ammonium nitrate as a catalyst in the synthesis of organic compounds is examined. Reactions that involve the generation of carbon-carbon bonds include electrophilic aromatic ...substitutions.
The combination of a three-component, solvent-free pyrrole synthesis performed under mechanochemical conditions with a TMSOTf-catalyzed oxonium-mediated cyclization gave general access to ...pyrrolo2,1-aisoquinoline derivatives under very mild conditions. The structural diversity generated by this method was extended by the preparation of six additional unusual polyheterocyclic frameworks.
We show that chiral effective field theory (EFT) two-body currents provide important contributions to the quenching of low-momentum-transfer Gamow-Teller transitions, and use chiral EFT to predict ...the momentum-transfer dependence that is probed in neutrinoless double-beta (0νββ) decay. We then calculate for the first time the 0νββ decay operator based on chiral EFT currents and study the nuclear matrix elements at successive orders. The contributions from chiral two-body currents are significant and should be included in all calculations.
In spite of advances in vaccination, control of the COVID-19 pandemic will require the use of pharmacological treatments against SARS-CoV2. Their development needs to consider the existence of two ...phases in the disease, namely the viral infection and the inflammatory stages. The main targets for antiviral therapeutic intervention are: (a) viral proteins, including the spike (S) protein characteristic of the viral cover and the viral proteases in charge of processing the polyprotein arising from viral genome translation; (b) host proteins, such as those involved in the processes related to viral entry into the host cell and the release of the viral genome inside the cell, the elongation factor eEF1A and importins. The use of antivirals targeted at host proteins is less developed but it has the potential advantage of not being affected by mutations in the genome of the virus and therefore being active against all its variants. Regarding drugs that address the hyperinflammatory phase of the disease triggered by the so-called cytokine storm, the following strategies are particularly relevant: (a) drugs targeting JAK kinases; (b) sphingosine kinase 2 inhibitors; (c) antibodies against interleukin 6 or its receptor; (d) use of the traditional anti-inflammatory corticosteroids.
Multicomponent reactions are one of the most interesting concepts in modern synthetic chemistry and, as shown in this critical review, they provide an attractive entry into pyrrole derivatives, which ...are very important heterocycles from many points of view including medicinal and pharmaceutical chemistry and materials science (97 references).
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