Methodology-driven efficient synthesis of cytotoxic (±)-piperarborenine B
The evolution of synthetic design toward the efficient synthesis of cyclobutane natural product (±)-piperarborenine B is demonstrated. Taking the advantages of good functional group compatibility of contractive synthesis of cyclobutanes from pyrrolidines,
Chunngai Hui, Andrey P. Antonchick
doaj +1 more source
This study introduces a tree‐based machine learning approach to accelerate USP8 inhibitor discovery. The best‐performing model identified 100 high‐confidence repurposable compounds, half already approved or in clinical trials, and uncovered novel scaffolds not previously studied. These findings offer a solid foundation for rapid experimental follow‐up,
Yik Kwong Ng +4 more
wiley +1 more source
A general protocol to afford enantioenriched linear homoprenylic amines [PDF]
The reaction of a readily obtained chiral branched homoprenylamonium salt with a range of aldehydes, including aliphatic substrates, affords the corresponding linear isomers in good yields and enantioselectivities.We thank the Spanish Ministerio de ...
Bosque, Irene +2 more
core +2 more sources
3-Hydroxypyrrolidine and (3,4)-dihydroxypyrrolidine derivatives: inhibition of rat intestinal α-glucosidase [PDF]
Thirteen pyrrolidine-based iminosugar derivatives have been synthesized and evaluated for inhibition of α-glucosidase from rat intestine. The compounds studied were the non-hydroxy, mono-hydroxy and dihydroxypyrrolidines.
Adriano, Gizé +8 more
core +1 more source
Three-Component Synthesis of Polysubstituted Homoproline Analogs
Tetrasubstituted pyrrolidines representing analogs of homoproline weresynthesized by three-component condensation of aryl(heteroaryl)aldehydes, asparagineand N-methylmaleimide (NMM). Compounds with (1S*, 3R*, 3aS*, 6aR*)-configurationat the corresponding
V. Irkha, K. Kudryavtsev
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NMR investigations of the interaction between the azo-dye sunset yellow and Fluorophenol [PDF]
The interaction of small molecules with larger noncovalent assemblies is important across a wide range of disciplines. Here, we apply two complementary NMR spectroscopic methods to investigate the interaction of various fluorophenol isomers with sunset ...
Aradi F. +51 more
core +1 more source
Carbohydrate-auxiliary assisted preparation of enantiopure 1,2-oxazine derivatives and aminopolyols
An approach to enantiopure hydroxylated 2H-1,2-oxazine derivatives is presented utilizing the [3 + 3] cyclisation of lithiated alkoxyallenes and an L-erythrose-derived N-glycosyl nitrone as precursors.
Marcin Jasiński +2 more
doaj +1 more source
Oxalates as Activating Groups for Alcohols in Visible Light Photoredox Catalysis: Formation of Quaternary Centers by Redox-Neutral Fragment Coupling. [PDF]
Alkyl oxalates are new bench-stable alcohol-activating groups for radical generation under visible light photoredox conditions. Using these precursors, the first net redox-neutral coupling of tertiary and secondary alcohols with electron-deficient ...
Jamison, Christopher R +4 more
core
ELECTROCHEMICAL REDUCTION OF 2,2,5,5-TETRAMETHYLPYRROLINE DERIVATIVES TO CORRESPONDING PYRROLIDINES
The reduction technique of 2,2,5,5-tetramethylpyrroline compounds to pyrrolidines on sodium amalgam preformed under the electrolysis of sodium hydroxide solution is described.
Irina Y. Zhukova +2 more
doaj
3-O-Benzhydryl-2,5-dideoxy-2,5-imino-2-C-methyl-l-lyxono-1,4-lactone
The title bicyclic lactone, C19H19NO3, is an intermediate in the synthesis of chiral α-methylprolines and branched C-methyl pyrrolidines; the absolute configuration was determined by the use of d-erythronolactone as the starting material.
David J. Watkin +3 more
doaj +1 more source

