Combination of multicomponent KA2 and Pauson-Khand reactions: short synthesis of spirocyclic pyrrolocyclopentenones was written by Innocenti, Riccardo;Lenci, Elena;Menchi, Gloria;Trabocchi, Andrea. And the article was included in Beilstein Journal of Organic Chemistry in 2020.Application In Synthesis of 1-Tosylpiperidin-4-one This article mentions the following:
The Cu-catalyzed multicomponent ketone-amine-alkyne (KA2) reaction was combined with a Pauson-Khand cycloaddition to give access of unprecedented constrained spirocyclic pyrrolocyclopentenone derivatives such as I [R1 = 3-thienyl, Ph; R2 = Ac, Bz; X = CH2, CHMe, N-BOC] following a DOS couple-pair approach. The polyfunctional mol. scaffolds were tested on cyclopentenone reactivity to further expand skeletal diversity, demonstrating utility of this combined approach in generating novel spiro compounds as starting material for the generation of chem. libraries. The chemoinformatics characterization of newly-synthesized mols. gave evidence about structural and physicochem. properties with respect to a set of blockbuster drugs, and showed that such scaffolds are drug-like but more spherical and three-dimensional in character than the drugs. In the experiment, the researchers used many compounds, for example, 1-Tosylpiperidin-4-one (cas: 33439-27-9Application In Synthesis of 1-Tosylpiperidin-4-one).
1-Tosylpiperidin-4-one (cas: 33439-27-9) belongs to piperidine derivatives.Piperidine is a key saturated heterocyclic scaffold found in several of the top-selling small molecule pharmaceuticals and natural alkaloids, with a diverse range of biological activities. The piperidine and polyhydroxylated indolizidine derivatives have shown to be promising α-glucosidase inhibitors. The former are analogs of DNJ with an improved α-glucosidase inhibitory profile than that of DNJ. Boisson et al.Application In Synthesis of 1-Tosylpiperidin-4-one
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem