Results 81 to 90 of about 18,532 (197)

Synthetic entry to functionalised morpholines and [1,4]-oxazepanes via reductive amination reactions of carbohydrate derived dialdehydes

, 2004
The rapid synthesis of functionalised morpholines and [1,4]-oxazepanes displaying up to three stereocentres, by reductive amination reactions between carbohydrate derived dialdehydes and a range of amines, is described. (C) 2004 Elsevier Ltd.
Clark, S.M., Osborn, H.M.I.
core   +1 more source

Chemoproteomic discovery of a brain‐penetrant, covalent NLRP3 inhibitor that binds a novel allosteric pocket

British Journal of Pharmacology, Volume 183, Issue 22, Page 6718-6734, November 2026.
NLRP3 is a promising inflammatory target, but existing inhibitors lack diversity and brain penetrance, and none are approved. Using chemoproteomics, we discovered a novel series that binds to Cys463 in a previously uncharacterized pocket. Compounds showed nanomolar potency, brain exposure, and in vivo suppression of IL‐1β, supporting neuroinflammatory ...
Donald C. Rogness, Evelyn P. Sievert, Vincent F. Vartabedian, Steffen M. Bernard, Erick Aitchison, William Tao, Mikaela Lindvall, Jing Qian, Christie L. Eissler, Brian E. Nordin, Benjamin D. Horning, Cian Kingston, Kelsey N. Lamb, Joshua C. Bell, Bingwen Lu, Jonathan Pollock, Jun Shi, Roli Khattri, David S. Weinstein, Matthew P. Patricelli, Brian N. Cook, Gabriel M. Simon   +21 more
wiley   +1 more source

Ruthenium‐Catalyzed Nitrile‐Acrylate Reductive Coupling by 2‐Propanol: Synthesis of Enantioenriched β‐Amino Esters

Angewandte Chemie, Volume 138, Issue 42, 12 October 2026.
The first nitrile reductive couplings beyond stoichiometric metals or metalloids are described. Using a ruthenium catalyst derived from RuHCl(CO)(PPh3)3 and Cy‐BIPHEP, 2‐propanol‐mediated reductive coupling of phenyl acrylate with aromatic or aliphatic nitriles delivers α,β‐unsaturated β‐amino esters.
Sebastian Höthker, Colin E. Hayter, Weijia Shen, Michael J. Krische   +3 more
wiley   +2 more sources

Facile Route to 3,5-Disubstituted Morpholines:  Enantioselective Synthesis of O-Protected trans-3,5-Bis(hydroxymethyl)morpholines

, 2016
trans-3,5-Bis(benzyl/tert-butyldiphenylsilyloxymethyl)morpholines, promising candidates for the C2-symmetric class of chiral reagents, were prepared with excellent optical purity. A key step in the synthesis is the coupling of a serinol derivative with 2,
N. André Sasaki (2654302), Rajesh Dave (2727565)   +1 more
core   +1 more source

4‐Thiazolidinone/2,4‐Thiazolidinedione–Sulfonamide Hybrids: A Concise Review of Their Design and Pharmacological Significance

ChemMedChem, Volume 21, Issue 20, 28 October 2026.
Sulfonamide–thiazolidinone hybrids integrate complementary pharmacophores to generate multifunctional scaffolds with broad pharmacological potential. Their structural versatility supports antimicrobial, antifungal, antioxidant, anticancer, anti‐inflammatory, antidiabetic, anticonvulsant, and enzyme‐inhibitory activities.
Subham Kumar Vishwakarma, Andressa Francielli Bonjorno, Sukhwant Singh, Christian S. Carnero Canales, Jean Leandro dos Santos, Cesar Augusto Roque‐Borda, Fernando Rogério Pavan   +6 more
wiley   +1 more source

Practical One‐Pot Synthesis of Cyclic Conjugated Amides From Ketones

European Journal of Organic Chemistry, Volume 29, Issue 40, 27 October 2026.
Cyclic conjugated amides from simple ketones: a one‐pot bromoform‐mediated homologation/amidation sequence provides direct access to 20 conjugated amides, including functionalized and linear examples, in up to 91% yield. Conjugated amides are valuable building blocks in organic synthesis; however, general access to cyclic conjugated amides remains ...
Maximilian Voigtländer, Johannes F. Teichert   +1 more
wiley   +1 more source

Photocatalyst‐Free Hydrodifluoromethylation of Alkenes via Thiol‐Mediated Photoactivation of Zn(CF2H)2(DMPU)2

Advanced Synthesis &Catalysis, Volume 368, Issue 20, 16 October 2026.
Herein, we report a photocatalyst‐free hydrodifluoromethylation of alkenes using Zn(CF2H)2(DMPU)2 and thiophenols under 390 nm irradiation. The thiophenol serves a dual stoichiometric function, promoting the formation of a photoactive thiol‐modified organozinc species while acting as the terminal hydrogen‐atom donor.
Hyunsu Kim, Seonyoung Kim, Hyunwoo Kim
wiley   +1 more source

Enantioselective Chemoenzymatic Synthesis of cis- and trans-2,5-Disubstituted Morpholines

, 2016
A versatile synthesis of enantiomerically pure cis- and trans-2,5-disubstituted morpholines is described. Hydroxynitrile lyase-mediated cyanide addition onto aldehydes provided cyanohydrins in virtually quantitative yield and excellent enantioselectivity.
Bas Ritzen (1980514), Elena Durán Verdasco (2297320), Floris L. van Delft (1261002), Steven Hoekman (1370907), Floris P. J. T. Rutjes (1450666)   +4 more
core   +1 more source

Visible‐Light Cobalt‐Catalyzed Synthesis of Aroyl Amides From Arylazo Sulfones

Advanced Synthesis &Catalysis, Volume 368, Issue 20, 16 October 2026.
Blue Light and Cobalt Catalysis for Synthesis! A versatile strategy that combines photoactive arylazo sulfones as substrates and Co2(CO)8 as a catalyst for the preparation of aromatic amides is presented herein. A versatile strategy leveraging the peculiar reactivity of arylazo sulfones as substrates bearing dyedauxiliary groups in arylation processes,
Komal Jaiswal, Lorenzo Di Terlizzi, Burkhard König, Maurizio Fagnoni, Stefano Protti   +4 more
wiley   +1 more source

Synthesis, Antiparasitic Activity, and ADME Profile of Morpholinephenylbenzamides: A Pharmacological Study Against Chagas Disease and Visceral Leishmaniasis

ChemMedChem, Volume 21, Issue 19, 14 October 2026.
Hit‐to‐lead optimization of morpholinephenylbenzamides reveals key structure–activity relationships against Trypanosoma cruzi and Leishmania infantum. Potency, selectivity, and ADME properties are differentially improved across the series, identifying compounds 20, 24, and 16 as complementary templates for the future design of dual antiparasitic leads.
Danilo Nascimento Farago, Daniela de Melo Resende, Mariza Gabriela Faleiro de Moura Lodi Cruz, Rafaela Marçal Sousa, Rafael Consolin Chelucci, Simone Michelan‐Duarte, Felipe da Silva Mendonça de Melo, Douglas Davison da Silva Oliveira, Paula Derksen Macruz, Alexandra Maria dos Santos Carvalho, Eduardo Jorge Pilau, Izabela Marques Dourado Bastos, Adriano D. Andricopulo, Leonardo L. G. Ferreira, Silvane Maria Fonseca Murta, Celso de Oliveira Rezende Júnior   +15 more
wiley   +1 more source