Pyrrolidine synthesis via ring contraction of pyridines [PDF]
A ring contraction of easily available cyclic compounds to smaller cycles that are valuable but difficult to synthetically access is one of important skeletal editing strategies.
Ryoga Ueno, Shohei Hirano, Jun Takaya
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HFIP-assisted Brønsted acid-catalyzed ring opening of 1-azabicyclo[1.1.0]butane to access diverse C3-quaternary aza-azetidines and indole-azetidines [PDF]
Nitrogen-based heterocycles represent 60% of small-molecule-approved drugs. Increasing demand for sp3-rich N-heterocyclic scaffolds as a bioisosteric replacement in drug discovery platforms has continued to drive the development of elegant methods for ...
Subrata Hazra +6 more
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3-(3-Azabicyclo[2, 2, 1]heptan-2-yl)-1,2,4-oxadiazoles as Novel Potent DPP-4 Inhibitors to Treat T2DM [PDF]
Background: Type 2 diabetes mellitus (T2DM) is a prevalent metabolic disease with global implications, necessitating effective management strategies.
Tatiana V. Zinevich +7 more
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Study of Cytotoxicity of Spiro-Fused [3-Azabicyclo[3.1.0]hexane]oxindoles and Cyclopropa[a]pyrrolizidine-oxindoles Against Tumor Cell Lines [PDF]
Background: A series of spiro-fused heterocyclic compounds containing cyclopropa[a]pyrrolizidine-2,3′-oxindole and 3-spiro[3-azabicyclo[3.1.0]-hexane]oxindole frameworks were synthesized and studied for their in vitro antiproliferative activity against ...
Anton A. Kornev +4 more
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Functional Activity of Enantiomeric Oximes and Diastereomeric Amines and Cyano Substituents at C9 in 3-Hydroxy-N-phenethyl-5-phenylmorphans [PDF]
The synthesis of stereochemically pure oximes, amines, saturated and unsaturated cyanomethyl compounds, and methylaminomethyl compounds at the C9 position in 3-hydroxy-N-phenethyl-5-phenylmorphans provided μ-opioid receptor (MOR) agonists with varied ...
Hudson G. Roth +8 more
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Synthesis and Antiprotozoal Activity of Azabicyclo-Nonane Pyrimidine Hybrids
2,4-Diaminopyrimidines and (dialkylamino)azabicyclo-nonanes possess activity against protozoan parasites. A series of fused hybrids were synthesized and tested in vitro against pathogens of malaria tropica and sleeping sickness.
Clemens Hinteregger +6 more
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3-Azabicyclo[3.1.0]hexanes are common structural components in natural products and bioactive compounds. Traditionally, the metal-mediated cyclopropanation domino reaction of chain enzymes is the most commonly used strategy for the construction of this ...
Jingya Li +5 more
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Selective Synthesis of N-Acylnortropane Derivatives in Palladium-Catalysed Aminocarbonylation
The aminocarbonylation of various alkenyl and (hetero)aryl iodides was carried out using tropane-based amines of biological importance, such as 8-azabicyclo[3.2.1]octan-3-one (nortropinone) and 3α-hydroxy-8-azabicyclo[3.2.1]octane (nortropine) as N ...
László Kollár +3 more
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Synthesis and Characterization of Two Schiff Base Tetradentate Ligands and their Related Complexes of [PDF]
:The compound [H2L1] (2,6-di(phenyl-4-methyl) [3.3.1] azabicyclo-9-2-amino ethylimine) was used to prepare two novel Schiff base ligands 2,4-bis [2,6-di(phenyl-4-methyl)[3.3.1] azabicyclo-9- 2-imine ethylimine] butane [L2] and 2,5-bis [2,6-di(phenyl-4 ...
Mahmoud S. muter
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Two modifications of previous procedures enabled the high-yield scalable synthesis of the pharmacologically important enantiomers of a C9-keto-5-phenylmorphan ((1R,5R)- and (1S,5S)-5-(3-methoxyphenyl)-2-methyl-2-azabicyclo[3.3.1]nonan-9-one).
Agnieszka Sulima +4 more
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