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Combinatorial chemistry

Papers (29)

Diels–Alder Polar Reactions of Azaheterocycles: A Theoretical and Experimental Study

Carla M. Ormachea, María Nélida Kneeteman & Pedro M. E. Mancini · Organics · 2022

A number of azaheterocycles (pyridines, pyrroles and indoles) have been properly functionalized so that they can act as dienophiles in cycloaddition Diels–Alder processes. This work analyzed the reactive behavior of these molecules through mechanistic analysis and the regioselect...

Open access Research Article 10.3390/org3020008

Stabilized Arylzinc Iodides in Negishi Acylative Cross-Coupling: A Modular Synthesis of Chalcones

Michele Pierigé, Anna Iuliano, Gaetano Angelici & Gianluca Casotti · Organics · 2022

Stabilized arylzinc iodides, synthesized by direct insertion of zinc into the corresponding halides, were used as nucleophiles into an acylative Negishi coupling reaction to synthesize chalcones. The reaction conditions were optimized to afford optimal results on a model reaction...

Open access Research Article 10.3390/org3020006

β-Cyclodextrin Supramolecular Recognition of bis-Cationic Dithienylethenes

Giulio Bianchini, Mattia Bazan, Fabrizio Fabris & Alessandro Scarso · Organics · 2022

The supramolecular interactions in water between β-cyclodextrin and the open and closed photochromic forms of two bis-cationic dithienylethenes, characterized by different electronic properties, were investigated aiming at underlying the key aspects of the recognition process. Th...

Open access Research Article 10.3390/org3020005

1-(4-Nitrophenyl)-1H-1,2,3-Triazole-4-carbaldehyde: Scalable Synthesis and Its Use in the Preparation of 1-Alkyl-4-Formyl-1,2,3-triazoles

Tomas Opsomer, Kaat Valkeneers, Ana Ratković & Wim Dehaen · Organics · 2021

1,2,3-Triazole-4-carbaldehydes are useful synthetic intermediates which may play an important role in the discovery of novel applications of the 1,2,3-triazole moiety. In this work, a one-step multigram scale synthesis of 4-formyl-1-(4-nitrophenyl)-1H-1,2,3-triazole (FNPT) as a p...

Open access Research Article 10.3390/org2040024

Boranils: Versatile Multifunctional Organic Fluorophores for Innovative Applications

Julien Massue, Denis Jacquemin & Gilles Ulrich · Organics · 2021

Multifunctional stimuli-responsive fluorophores showing bright environment-sensitive emissions have fueled intense research due to their innovative applications in the fields of biotechnologies, optoelectronics, and materials. A strong structural diversity is observed among molec...

Open access Research Article 10.3390/org2040020

Recent Advances in the Synthesis of Piperazines: Focus on C–H Functionalization

Carolina Durand & Michal Szostak · Organics · 2021

Piperazine ranks as the third most common nitrogen heterocycle in drug discovery, and it is the key component of several blockbuster drugs, such as Imatinib (also marketed as Gleevec) or Sildenafil, sold as Viagra. Despite its wide use in medicinal chemistry, the structural diver...

Open access Research Article 10.3390/org2040018

Synthesis of 1-Trifluorometylindanes and Close Structures: A Mini Review

Olesya V. Khoroshilova & Aleksander V. Vasilyev · Organics · 2021

This review describes methods for the synthesis of 1-trifluomethylindanes and close structures, which are still quite rare and scarcely available compounds. There are two main approaches to obtain 1-CF3-indanes. The first one is the construction of an indane system from CF3 precu...

Open access Research Article 10.3390/org2040019

Electrocyclizations of Conjugated Azapolyenes Produced in Reactions of Azaheterocycles with Metal Carbenes

Nikolai V. Rostovskii, Mikhail S. Novikov & Alexander F. Khlebnikov · Organics · 2021

Conjugated azapolyenes (azabuta-1,3-dienes, aza-/diaza-/oxaza-/oxadiazahexa-1,3,5-trienes) are highly reactive in electrocyclization reactions, which makes them convenient precursors for the synthesis of a wide range of four-, five-, and six-membered nitrogen heterocycles that ar...

Open access Research Article 10.3390/org2030017

Ring-Opening of Cyclodextrins: An Efficient Route to Pure Maltohexa-, Hepta-, and Octaoses

Matthieu Pélingre, Dindet Steve-Evanes Koffi Teki, Jamal El-Abid, Vincent Chagnault, José Kovensky & Véronique Bonnet · Organics · 2021

Many preparations of maltooligosaccharides have been described in literature, essentially using enzymatic or biotechnological processes. These compounds, derived from starch, are well-known as prebiotic agents. The use of maltohexa-, hepta-, and octaoses as synthons in organic sy...

Open access Research Article 10.3390/org2030015

Design, Synthesis, and Utility of Defined Molecular Scaffolds

Daisuke Sato, Zhiyuan Wu, Hikaru Fujita & Jonathan Lindsey · Organics · 2021

A growing theme in chemistry is the joining of multiple organic molecular building blocks to create functional molecules. Diverse derivatizable structures—here termed “scaffolds” comprised of “hubs”—provide the foundation for systematic covalent organization of a rich variety of...

Open access Research Article 10.3390/org2030013

A Review of the Synthetic Strategies toward Dihydropyrrolo[1,2-a]Pyrazinones

Pieterjan Winant, Tomas Horsten, Shaiani Gil de Melo, Flavio Emery & Wim Dehaen · Organics · 2021

Dihydropyrrolo[1,2-a]pyrazinone rings are a class of heterocycles present in a wide range of bioactive natural products and analogues thereof. As a direct result of their bioactivity, the synthesis of this privileged class of compounds has been extensively studied. This review pr...

Open access Research Article 10.3390/org2020011

A Sustainable Improvement of ω-Bromoalkylphosphonates Synthesis to Access Novel KuQuinones

Mattia Forchetta, Valeria Conte, Giulia Fiorani, Pierluca Galloni & Federica Sabuzi · Organics · 2021

Owing to the attractiveness of organic phosphonic acids and esters in the pharmacological field and in the functionalization of conductive metal-oxides, the research of effective synthetic protocols is pivotal. Among the others, ω-bromoalkylphosphonates are gaining particular att...

Open access Research Article 10.3390/org2020010

α-(Imino)pyridyldifluoroethyl Phosphonates: Novel Promising Building Blocks in Synthesis of Biorelevant Aminophosphonic Acids Derivatives

Oksana Shavrina, Lyudmyla Bezgubenko, Andrii Bezdudny, Petro Onys’ko & Yuliya Rassukana · Organics · 2021

A convenient synthetic approach to previously unknown NH-iminophosphonates bearing 2-, 3-, and 4-pyridyldifluoromethyl groups at the imine carbon atom was developed. The synthetic potential of these novel building blocks was demonstrated by their conversion into highly functional...

Open access Research Article 10.3390/org2020007