Synonyms:2-azetidinone;4-carboxy-2-azetidinone;azetidinone
98% *data from raw suppliers
2-Azetidinone *data from reagent suppliers
C
There total 40 articles about 2-Azetidinone which guide to synthetic route it. The literature collected by LookChem mainly comes from the sharing of users and the free literature resources found by Internet computing technology. We keep the original model of the professional version of literature to make it easier and faster for users to retrieve and use. At the same time, we analyze and calculate the most feasible synthesis route with the highest yield for your reference as below:
Reference yield: 95.6%
Reference yield: 80.0%
Reference yield: 61.0%
The research focuses on the efficient green synthesis of Schiff bases and azetidinones derivatised with 1,2,4-triazoles. The study employs Mg(ClO4)2 as a catalyst for the synthesis of Schiff bases from 1-amino-2-aryl-3-oxo-1,2,4-triazoles with various aldehydes under solvent-free conditions. The resulting Schiff bases are then reacted with chloroacetyl chloride to yield azetidinones, also in solvent-free conditions, with excellent yields. The synthesized compounds were analyzed for their potential as drugs by evaluating properties such as penetration into biological membranes (clogP), drug-likeliness, and drug scores. Additionally, the compounds were screened for antitubercular and antimicrobial activities. The analyses included techniques such as IR spectroscopy, 1H NMR spectroscopy, mass spectrometry, and elemental analysis, as well as thin layer chromatography (TLC) to check the purity of the compounds. The pharmacological evaluation was carried out at a separate facility, and the OSIRIS property explorer was used for computational drug analysis.
The research focuses on the synthesis of structurally diverse 2-azetidinones, which are key structural elements in the family of β-lactam antibiotics and possess significant biological activities. The study aims to develop a new method for the synthesis of β-lactams via ketene-imine cycloaddition using polymer-supported ketene on a solid support, specifically Merrifield resin. The researchers successfully synthesized a variety of β-lactam derivatives with different substituents at positions 1 and 4, which could serve as potential intermediates for the synthesis of active compounds. The process involved the use of trimellitic anhydride, phthaloylglycine, imines, Vilsmeier reagent, triethylamine, trifluoroacetic acid, methylhydrazine, and other reagents. The conclusions of the research highlight the selective cleavage of supported β-lactams by trifluoroacetic acid and methylhydrazine to obtain 4-carboxyphthalimido- and 3-amino-β-lactams, respectively. The method offers simplified purification through filtration, avoiding time-consuming separation techniques, and the ability to regenerate the starting polymer-supported phthaloylglycine, making it a valuable contribution to solid-phase polymer-supported synthesis.
The research aims to develop a highly efficient and stereoselective method for constructing chiral four-membered ring compounds, specifically β-lactams and cyclobutanones, which are important in pharmaceuticals and natural products. The study employs an iridium (Ir) catalyst complexed with an axially-unfixed biphenyl phosphine-oxazoline ligand (BiphPHOX) to achieve asymmetric hydrogenation under mild conditions (1.0 - 2.5 bar H? for 1.0 - 10 hours). The reaction conditions were optimized to achieve excellent yields (up to 99%) and enantioselectivities (up to 98%). The study concludes that this method is highly efficient, with a wide substrate scope and potential for further transformations, making it a valuable protocol for the synthesis of chiral four-membered ring compounds.
The study focuses on the design and synthesis of fluorescent analogues of cholesterol absorption inhibitors (CAIs), specifically those related to the 2-azetidinone class, such as Sch 58235. The researchers aimed to create single enantiomer fluorescent CAIs to investigate the mechanism of action (MOA) of these inhibitors. They initially synthesized a benzothiadiazole-containing analogue (7) and its glucuronide (8), but found the fluorescence too dim for detailed binding studies. Subsequent efforts involved creating analogues with fluorescein-like properties using palladium coupling technology, resulting in compound 14, which was abandoned due to sensitivity issues. Finally, they used a BODIPY moiety to produce a stable, highly fluorescent CAI (16) with suitable biological activity. All synthesized compounds were tested in a rapid cholesterol absorption assay in rats, confirming their potency as CAIs and suitability for MOA studies.
The research focused on the optimization, design, and synthesis of T-type calcium channel blockers, specifically spiropiperidine azetidines and azetidinones, with the goal of treating inflammatory and neuropathic pain. The research involved a series of experiments to evaluate and optimize the potency, selectivity, and drug metabolism and pharmacokinetic (DMPK) properties of these blockers targeting CaV3.2 channels. The experiments utilized a modular synthetic approach to explore structure-activity relationships (SAR) using a variety of reactants, including esters, aldimines, and isocyanates. Analytical techniques such as IonWorks HT, manual patch clamp analysis, and whole-cell patch clamp analysis were used to evaluate the activity and selectivity of the synthesized compounds. The research also endeavored to improve DMPK properties and TRPV1 selectivity through structural modifications, and in vivo evaluations were performed using a rat spinal nerve ligation model to assess the efficacy of the compounds in treating neuropathic pain. Although the compounds showed good in vitro activity, they did not show statistically significant effects in in vivo models, which was attributed to high protein binding and the need for higher in vivo exposures to effectively block CaV3.2 channels.
The first study highlights the efficiency of pig liver esterase in producing optically active intermediates and the potential for synthesizing chiral ?-amino acids.The second study emphasizes the versatility and efficiency of the Ph3P-(PyS)2-CH3CN system under neutral conditions.The third study investigates the inhibitory effects of a synthesized 25-aza derivative on the enzyme (S)-adenosyl-L-methionine:cycloartenol C-24-methyltransferase. The compound, 24-methyl-25-azacycloartanol, was found to be a potent inhibitor with a high affinity for the enzyme, suggesting its potential as a tool for studying enzyme mechanisms and possibly for pharmaceutical applications.
The research focuses on a novel synthesis method for β-lactam compounds, which are important in pharmaceutical applications. The purpose of the study was to explore the behavior of spirocyclopropane isoxazolidines under different conditions, specifically with strong acids, to develop a new route for synthesizing valuable β-lactam derivatives. The researchers used readily available and inexpensive anthranilic acid as a starting material, employing tosyl (Ts) and nosyl (2-nitrobenzenesulfonyl, Ns) groups to protect the amino acid nitrogen atom. The process involved the preparation of alkylidenecyclopropanes through palladium(0) catalysis, followed by conversion to isoxazolidines and subsequent heating in the presence of trifluoroacetic acid (TFA) or other strong acids.
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