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5th International Symposium on Synthesis and Catalysis (ISySyCat2023)

Carreiro, Elisabete; Burke, Anthony

In this thematic issue dedicated to the 5th International Symposium on Synthesis and Catalysis (ISySyCat2023), which took place in Evora, Portugal from September 5–8, 2023, a diverse selection of contributions from a cross section of these participants is presented. The variety of material from different fields showcased in this thematic issue truly reflects the range and breath of this conference.


Assessing the Potential of 1,2,3-Triazole-Dihydropyrimidinone Hybrids against C...

Carreiro, Elisabete; Costa, Ana; Burke, Anthony; Antunes, Célia; Gastalho, Carlos; Pereira, Florbela; Lopez, Oscar; Fernández-Bolaños, José G.

Combining the pharmacological properties of the 1,2,3-triazole and dihydropyrimidinone classes of compounds, two small families of mono- and di(1,2,3-triazole)-dihydropyrimidinone hybrids, A and B, were previously synthesized. The main objective of this work was to investigate the potential anti-Alzheimer effects of these hybrids. The inhibitory activities of cholinesterases (AChE and BuChE), antioxidant activi...


Asymmetric Additions Empowered by OrganoCatalysts, Metal Catalysts, and Natural...

Carreiro, Elisabete; Burke, Anthony; Hermann, Gesine; Federsel, H.-J.

This article is a history of an industrial–academic partnership that started almost two decades ago and details the evolution of a relationship between a small academic research group and a spin-out company located in Portugal. Their activities have ranged from the development of new metal-based catalytic systems for asymmetric epoxidations, allylic alkylations, and arylations to the development of novel cincho...


Stereoselective Catalytic Synthesis of Bioactive Compounds in Natural Deep Eute...

Carreiro, Elisabete; Burke, Anthony; Hermann, Gesine; Federsel, H.-J.

Deep eutectic solvents (DESs) are a mixture of two or more components, and at a particular composition, they become liquids at room temperature. When the compounds that constitute the DESs are primary metabolites namely, amino acids, organic acids, sugars, or choline derivatives, the DESs are called natural deep eutectic solvents (NADESs). NADESs fully represent green chemistry principles. These solvents are hi...


Asymmetric Additions Empowered by OrganoCatalysts, Metal Catalysts, and Deep Na...

Carreiro, Elisabete; Burke, Anthony; Federsel, H.-J.; Hermann, Gesine

This article is a history of an industrial−academic partnership that started almost two decades ago and details the evolution of a relationship between a small academic research group and a spin-out company located in Portugal. Their activities have ranged from the development of new metal-based catalytic systems for asymmetric epoxidations, allylic alkylations, and arylations to the development of novel cincho...


Amino acids as chiral building blocks

Carreiro, Elisabete P.; Burke, Anthony

This chapter is focused on the application of amino acids as building blocks in asymmetric synthesis. As a tool for accessing enantiopure compounds, amino acids have been used in four different ways, (i) as chiral precursors, (ii) as chiral reagents, (iii) as chiral auxiliaries, and (iv) as organocatalysts. For decades amino acids, particularly α-amino acids, have been used consistently for the synthesis of num...


Immobilization of Functionalized epi-Cinchonine Organocatalysts on Controlled P...

Carreiro, Elisabete; Amorim, Ana; Fonseca, Daniela; Burke, Anthony; Hermann, Gesine; Federsel, H-J

A well-known squaramide-cinchonine organocatalyst was immobilized in a controlled way onto three types of commercial porous glass beads EziG™ (EziG OPAL, EziG Amber, and EziG Coral) and applied in asymmetric Michael reactions. The performance of the immobilized catalysts was evaluated under batch and continuous-flow conditions, showing promising results in both approaches. In batch reactions, 0.8 and 1.6 mol% o...


cEpiderm, a Canine Skin Analog Suitable for In Vivo Testing Replacement

Marques, Mariana; Nunes, João; Ustymenko, Bárbara; Fialho, Luísa; Martins, Luís; Burke, Anthony; Filho, Cesar; Craveiro, Alexandre; Costa, Ana

Skin is one of the organs most tested for toxicity and safety evaluation during the process of drug research and development and in the past has usually been performed in vivo using animals. Over the last few years, non-animal alternatives have been developed and validated epidermis models for human and rat skin are already available. Our goal was to develop a histotypical canine skin analog, suitable for non-a...


Development of a canine epidermis equivalent model for evaluation of sensitization

Marques, M; Nunes, J; Ustymenko, B; Lagoa, Tânia; Fialho, Luísa; Martins, Luís; Burke, Anthony; Souza, E; Filho, César; Craveiro, Alexandre; Costa, Ana

Background Canine atopic dermatitis (cAD) is a genetic-predisposed allergic and pruritic inflammatory skin condition, associated with sensitization to environmental allergens. Keratinocytes can produce several inflammatory mediators, in response to several other host mediators, antigens, and pathogens by virtue of their wide range of surface receptors, some of them dysregulated in cAD individuals. A histotypica...


Stereoselective Benzilic Acid Rearrangements: New Developments on an Old Story,

Burke, Anthony; Moutayakine, Amina

The benzilic acid rearrangement (BAR) is the oldest rearrangement on record. It is a powerful synthetic tool for accessing significant biologically active molecules. The reaction is both catalytic (generally Lewis acid) and stereoselective, recently the first catalytic asymmetric version was reported with astonshing results (ees of up to 97%) to give chiral tartronic esters. In this unique highlight, we look at...


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