Photochemical thiocarbonyl difluoride generation enables azetidine synthesis [PDF]
Nature CommunicationsThe activation of amines into thiocarbamoyl fluorides (TCarbFs) provides access to valuable nitrogen-based functionalities. However, their broader use has been hindered by the reliance on harsh reagents and conditions.
Ricardo I. Rodríguez +9 more
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Synthesis of 1,4-Benzodiazepines via Intramolecular C–N Bond Coupling and Ring Opening of Azetidines [PDF]
MoleculesA facile and efficient synthesis of functionalized 1,4-benzodiazepine derivatives under mild conditions was developed. The CuI/N,N-dimethylglycine-catalyzed intramolecular cross-coupling reaction of 1-(2-bromobenzyl)azetidine-2-carboxamides proceeded ...
Xin-Ming Xu +5 more
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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]
Nature CommunicationsNitrogen-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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Synthesis, Computational Studies, and Structural Analysis of 1-(3,5-Dimethoxyphenyl)azetidin-2-ones with Antiproliferative Activity in Breast Cancer and Chemoresistant Colon Cancer [PDF]
PharmaceuticalsBackground/Objectives: A series of 1-(3,5-dimethoxyphenyl)azetidine-2-ones were synthesised to evaluate their antiproliferative activity in MCF-7 breast cancer cells and HT-29 chemoresistant colon cancer cells. The 1,4-diarylazetidin-2-ones were designed
Azizah M. Malebari +6 more
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Molecular basis for azetidine-2-carboxylic acid biosynthesis [PDF]
Nature CommunicationsAzetidine-2-carboxylic acid (AZE) is a long-known plant metabolite. Recently, AZE synthases have been identified in bacterial natural product pathways involving non-ribosomal peptide synthetases.
Tim J. Klaubert +8 more
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Synthesis of Azetidine-Based Beta-Amino Alcohols
Medical Sciences Forum, 2022 Beta-amino alcohols are versatile chemicals used as scaffolds in medicinal chemistry and they are key factors for the efficacy of numerous pharmaceutical products.
Linda Supe
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trans-3-Benzyloxycarbonylamino-1-methyl-3-(methylcarbamoyl)azetidine-1-oxide
Molbank, 2023 trans-3-Benzyloxycarbonylamino-1-methyl-3-(methylcarbamoyl)azetidine-1-oxide was prepared by stereoselective oxidation of the corresponding azetidine precursor.
Dayi Liu +3 more
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Molecules, 2021 Photocycloreversion plays a central role in the study of the repair of DNA lesions, reverting them into the original pyrimidine nucleobases. Particularly, among the proposed mechanisms for the repair of DNA (6-4) photoproducts by photolyases, it has been
Miriam Navarrete-Miguel +4 more
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Frontiers in Chemistry, 2023 Azetidine is a prevalent structural motif found in various biologically active compounds. In this research paper, we report La(OTf)3-catalyzed intramolecular regioselective aminolysis of cis-3,4-epoxy amines to afford azetidines.
Yuse Kuriyama +2 more
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Methyl 2-Amino-4-[1-(tert-butoxycarbonyl)azetidin-3-yl]-1,3-selenazole-5-carboxylate
Molbank, 2021 Methyl 2-amino-4-[1-(tert-butoxycarbonyl)azetidin-3-yl]-1,3-selenazole-5-carboxylate as a newly functionalized heterocyclic amino acid was obtained via [3+2] cycloaddition. The structure of the novel 1,3-selenazole was unequivocally confirmed by detailed
Karolina Dzedulionytė +5 more
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