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Showing 1 to 11 of 11 for “"azetidine"”.
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Preparation and Properties of Azetidine-2-Ones
The preparation and properties of some known azetidine~2-ones are reviewed, and the biological properties are summarised. A series of new azetidinones have been synthesised. The cycloaddition of diphenylketene or ketene to Schiff's bases yielded the 3,3-disubstituted and the 3-unsubstituted …
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Synthesis and Biological Evaluation of Novel GBR 12909 Tropane and Azetidine Hybrid Analogues
… of 3-[2-(diarylmethoxyethylidenyl)]-Nsubstituted azetidine derivatives has been developed.
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Synthesis and Biological Evaluation of Rigid Analogues of Methamphetamines
… <em>N</em>-Boc-azetidinone. The benzylideneazetidine analogs were prepared via a Wittig olefination via the ylides generated from the corresponding triphenylphosphonium benzylhalide salts. The substituted benzylazetidine analogs were synthesized from the corresponding benzylideneazetidienes …
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Synthesis Of Natural Product-Based Sphingosine Derivatives
… conditions. Natural products that consist of an azetidine ring represents an interesting class of conformationally constrained scaffolds that may serve as effective lead compounds for SK inhibitor development. Hence, the goal of this thesis research was to synthesize natural-product based …
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Synthesis, Vinylation and Rearrangement of NH-Isoxazolines and Copper Catalyzed 6 Pi Electrocyclization
… Chapter 2 discusses a ring expansion reaction of azetidine–N–oxides to form highly functionalized isoxazolidine products with up to 3 contiguous stereocenters in excellent diastereoselectivity. The scope was explored and shown to be tolerant for a wide array of aniline nucleophiles as well as a …
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New Strategies for the Synthesis of Amines, Ethers and Small Strained Rings
… advances made in the synthesis of spirocyclic NH-azetidine rings through a Ti(IV)-mediated Kulinkovich-type coupling of oxime ethers with primary alkyl Grignard reagents or terminal olefins. A significant development in this project is related to the purification and handling of the sensitive and …
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Mild [Pd(OAc)2/PPh3] catalyzed cyclization reactions of N-Alkyl-2-vinylazetidines with heterocumulenes.
A synthetic route to N-alkylated 2-vinylazetidines is presented, and highly regioselective methods for the palladium(0)-catalyzed insertion of heterocumulenes into these substrates have been established, employing a Pd(OAc)2/PPh3 catalyst system under very mild conditions. An assortment of …
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Synthesis of 4-(trifluoromethyl)azetidin-2-one building blocks and their transformation into novel CF3-substituted amines and heterocyclic systems
… ring opening or initial carbonyl removal to azetidine intermediates, followed by ring opening. In addition, hydrogenolysis of the benzylether fragment in 3-benzyloxy-4-trifluoromethyl-β-lactams resulted in the formation of 3-hydroxy-4-trifluoromethyl-β-lactams as a second class of new …
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Palladium-mediated C–H Functionalization of Aliphatic Amines via High Valent Palladium(IV) Intermediates
… intramolecular γ C–H amination process to form azetidine products from hindered cyclic amines. Following this, aryl halides containing coordinating groups at the ortho position were discovered as efficient palladacycle oxidants in which the ortho-group pre-coordinates to the palladium centre to …
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Synthesis, pharmacological and solubility evaluation of antiplasmodial pyrido[1,2-a]benzimidazoles with cyclic and functionalized amine side chain substituents
… lower solubility compared to the piperidines. Azetidine and cyclohexylamine substitution led to compounds with moderate to poor in vitro activity and solubility. Substitution with highly polar functions and reduced basicity of the second amino group on the cyclic amine moiety were found to be …
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Regulation of The Heat Shock Response By Thiol-Reactive Compounds In The Yeast Saccharomyces Cerevisiae
… of unfolded proteins, the proline analog azetidine-2-carboxylic acid (AZC) and protein cross-linker dithiobis(succinimidyl propionate) (DSP) were used to force misfolding of nascent polypeptides and existing cytosolic proteins, respectively. Both unfolding reagents display kinetic HSP …