Catalytic approaches towards heterocyclic aziridine and aryl ethylamine scaffolds [PDF]
Nitrogen-containing heterocyclic scaffolds are prevalent within bioactive molecules and natural products. Of these, aziridine scaffolds represent viable targets, both as bioactive molecules (e.g., as covalent inhibitors) but also as synthetic ...
Hilton, Timothy Alex
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Stereocontrolled Synthesis of 1,2- and 1,3-Diamine Building Blocks from Aziridine Aldehyde Dimers
Vicinal aziridine-containing diamines have been obtained with high syn-stereoselectivity from readily available aziridine aldehyde dimers in the Petasis borono-Mannich reaction.
Jeffrey D. St. Denis (1724728) +3 more
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Alkylative Ring-Opening of Bicyclic Aziridinium Ion and Its Application for Alkaloid Synthesis
Alkylative ring-opening of bicyclic aziridinium ion generated from 4-hydroxybutylaziridine with organocopper reagent was achieved successfully to afford 2-alkylsubstituted piperidine in high or moderate yield.
Nagendra Nath Yadav +3 more
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Solid phase synthesis of aziridine 2-carboxylates
Several oligopeptides and amino acids containing an aziridine 2-carboxylate group were prepared using a solid phase version of the Gabriel-Cromwell reaction.
Filigheddu, S. N. +2 more
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A New Self-Polymerization of Acrylic Acid with a Mono-aziridine Containing Compound
A new self-polymerization took place between acrylic acid (AA) and a mono-aziridine containing compound, e.g. methyl 3-(aziridin-1-yl) propanoate (MAP) upon mixing that resulted in formation of a linear polyethyleneimine (PEI) with amino-ester bonds ...
Chen, Kan-Nan +1 more
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Organocatalyzed enantioselective desymmetrization of aziridines and epoxides
Enantioselective desymmetrization of meso-aziridines and meso-epoxides with various nucleophiles by organocatalysis has emerged as a cutting-edge approach in recent years.
Ping-An Wang
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The Aziridine-Mediated Ligation and Efforts Towards a General Synthesis of N-terminal Aziridinyl Peptides [PDF]
Herein is described the Aziridine-Mediated Ligation's discovery, conceptual development, and the efforts to develop a general synthetic method for the synthesis of unprotected peptide chains terminated in an aziridine.
Dyer, Frank
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An hydroxypropyl-aziridine-containing side chain is attached to an oxonaphthalene-annelated pyrrole in expectation of DNA alkylating properties. The cytotoxicity is evaluated against two cell lines, KB-31 and KB-8511, respectively.
Christiane Puschmann, Helmut Spreitzer
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Salen–scandium(III) complex-catalyzed asymmetric (3 + 2) annulation of aziridines and aldehydes
Oxazolidine is one of the crucial structural moieties of biologically active compounds. A salen–scandium triflate complex-catalyzed asymmetric (3 + 2) annulation of dialkyl 1-sulfonylaziridine-2,2-dicarboxylates and aldehydes generated optically active ...
Linqiang Wang, Jiaxi Xu
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Metal-free one-pot synthesis of 2-substituted and 2,3-disubstituted morpholines from aziridines
The metal-free synthesis of 2-substituted and 2,3-disubstituted morpholines through a one-pot strategy is described. A simple and inexpensive ammonium persulfate salt enables the reaction of aziridines with halogenated alcohols to proceed via an SN2-type
Hongnan Sun +4 more
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