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Herein we report a series of telescoping methodologies for one pot synthesis of biologically relevant γ-carboline derivatives and spiro[pyrrolidinone-3,3']indole . Initially the three consecutive steps of cyclopropanation, phthalimide deprotection, and Boc-deprotection have been congregated in a single reaction vessel to afford a ∼1:1 mixture of and . Next, careful optimization of the reaction sequence and the conditions generated an orthogonal approach to access compounds and exclusively. Air oxidation of the γ-carbolinones afforded aromatic γ-carbolines .
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http://dx.doi.org/10.1021/acs.joc.1c00141 | DOI Listing |
Chem Sci
September 2025
Molecular AI, Discovery Sciences, BioPharmaceuticals R&D, AstraZeneca Gothenburg Sweden
Incorporating non-natural amino acids (NNAAs) into peptides enhances therapeutic properties, including binding affinity, metabolic stability, and half-life time. The pursuit of novel NNAAs for improved peptide designs faces the challenge of effective synthesis of these building blocks as well as the entire peptide itself. Solid-Phase Peptide Synthesis (SPPS) is an essential technology for the automated assembly of peptides with NNAAs, necessitating careful protection for effective coupling of amino acids in the peptide chain.
View Article and Find Full Text PDFmSphere
September 2025
Instituto de Tecnologia Química e Biológica António Xavier, Oeiras, Portugal.
Most strains of produce two toxins, TcdA and TcdB, which are mainly responsible for the disease symptoms. TcdA and TcdB are coded for by genes in the pathogenicity locus (PaLoc). Some epidemic strains, however, such as R20291, of ribotype 027, additionally produce a binary toxin, CDT, coded for by genes in the CDT locus (CdtLoc).
View Article and Find Full Text PDFChemistry
September 2025
Department of Chemistry, Indian Institute of Technology Kharagpur, Kharagpur, West Bengal, 721302, India.
Employing heterobimetallic complexes (HBCs) offers an exciting and powerful strategy for various catalytic applications. Here, we present an unorthodox synthetic route to synthesize a novel Ru-Fe heterobimetallic complex by implementing the strategy of "metalation with functionalization." This complex utilizes a redox-assisted concerted strategy to facilitate the controlled radical polymerization (CRP) of acrylate monomers with significantly low catalyst loading.
View Article and Find Full Text PDFGels
July 2025
Department of Plant Sciences, North Dakota State University, Fargo, ND 58108, USA.
To rationally utilize and develop agricultural waste products, this research involved the synthesis of degradable high water-absorbing resin through the graft copolymerization of cotton straw (CS) with monomers. Among them, acrylic acid (AA) and acrylamide (Am) are used as grafting copolymer monomers, cellulose in the straw serves as the network framework, and MBA acts as the crosslinking agent. Co gamma rays as initiators.
View Article and Find Full Text PDFJ Am Chem Soc
August 2025
Genomics Research Center, Academia Sinica, 128, Section 2, Academia Road, Taipei 11529, Taiwan.
Green algae, commonly used as a source of food nutrients, contain ulvan, which is a water-soluble sulfated heteropolysaccharide isolated from . Ulvan exhibits a range of biological properties, including antitumor, antiviral, anticoagulant, and immunomodulatory activities. Its sugar backbone consists of 1→4-linked disaccharide repeating units, which are categorized as ulvanobiuronic acids (types A and B) and ulvanobioses (types U and U).
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