- Solid phase synthesis of bicyclic pyrrolidines
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The preparation of bicyclic pyrrolidines, stable and easy to isolate, is performed through both classical solution chemistry and on solid support. A new linker strategy is presented based on the concept of REM resin approach. Starting from a suitably derivatized Wang's resin, the linker can be REgenerated after cleavage of the product and functionalized to start a new synthetic cycle via a Michael reaction. In the present work a vinyl sulfone supported on a Wang's resin is able to undergo a Michael reaction with an amino acid derivative; the obtained adduct serves as a precursor for azomethine ylide generation, which is conveniently trapped with N-methyl-maleimide. The results are presented and discussed in the light of the experimental conditions applied as well as the method chosen for the cleavage of the product and resin regeneration.
- Quadrelli, Paolo
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- Hydroxyethyl sulfone based reactive coalescing agents for low-VOC waterborne coatings
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The unique characteristics of water-based hydroxyethyl sulfone (HES)-vinyl sulfone (VS) dynamic equilibrium are exploited in the design of new reactive coalescing agents (RCAs) for the first time to address VOC (Volatile Organic Compound) emission issues
- Jana, Satyasankar,Kaur, Jagjit,Krishnan, Ranganathan,Ramalingam, Balamurugan
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p. 17171 - 17179
(2020/05/18)
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- Site-Selective Functionalization of Methionine Residues via Photoredox Catalysis
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Bioconjugation technologies have revolutionized the practice of biology and medicine by allowing access to novel biomolecular scaffolds. New methods for residue-selective bioconjugation are highly sought to expand the toolbox for a variety of bioconjugati
- Kim, Junyong,Li, Beryl X.,Huang, Richard Y.-C.,Qiao, Jennifer X.,Ewing, William R.,Macmillan, David W. C.
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supporting information
p. 21260 - 21266
(2020/12/21)
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- SULFOXIMINE DERIVATIVES AS FACTOR XA INHIBITORS
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The present invention relates to novel substituted sulfoximine derivatives of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their pre
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Page/Page column 20
(2011/04/18)
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- OXIDISED SULFURATED DISTAMYCIN DERIVATIVES, PROCESS FOR PREPARING THEM, AND THEIR USE AS ANTITUMOR AGENTS
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Compounds which are oxidised sulfurated distamycin derivatives of formula (I) wherein n is 2, 3 or 4; c is 1 or 2; A is a bond, a C1-C4 alkylene or C2-C4 alkenylene group; R1 and R2, which are the same or different, are selected from hydrogen, C1-C4 alkyl
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- COMBINATORIAL ACTIVE COMPOUND SYNTHESIS AND ITS INTERMEDIATES
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The invention relates to a resin-bound synthesis process for the preparation of chemical compounds of the formula (I) R1—SO2—NH—CO—R2??(I) in which R1 and R2 each are an organic radical, which compris
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- Phenyl sulfur mustard derivatives of distamycin A
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The design, synthesis, and cytotoxic activity of novel benzoyl and cinnamoyl sulfur mustard derivatives of distamycin A are described and structure-activity relationships are discussed. These sulfur mustards are more potent cytotoxics than corresponding nitrogen mustards in spite of the lower alkylating power, while their sulfoxide analogues are substantially inactive. Cinnamoyl sulfur mustard derivative (7) proved to be one of the most active distamycin-derived cytotoxics, about 1000 times more potent than melphalan. (C) 2000 Elsevier Science Ltd. All rights reserved.
- Cozzi, Paolo,Beria, Italo,Caldarelli, Marina,Capolongo, Laura,Geroni, Cristina,Mazzini, Stefania,Ragg, Enzio
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p. 1653 - 1656
(2007/10/03)
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- The CAMET and CASET Links for the Synthesis of Protected Oligopeptides and Oligodeoxynucleotides on Solid and Soluble Supports
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Simple bifunctional carboxy- and phospho-protecting groups are described which allow the attachment of protected amino acids and nucleotides to soluble or insoluble carriers.After chemical synthesis with conventional procedures, the completed oligopeptide
- Schwyzer, Robert,Felder, Eduard,Failli, Paola
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p. 1316 - 1327
(2007/10/02)
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- A NEW SOLID PHASE APPROACH FOR RAPID SYNTHESES OF OLIGONUCLEOTIDES BEARING A 3'-TERMINAL PHOSPHATE GROUP
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Synthesis of pentanucleotide ApTpCpTpTp containing a 3'-terminal phosphomonoester group was accomplished with the help of the new phosphate-solid phase link 2-(4-carboxyphenylmercapto)ethanol; a similar molecule, 2-benzylsulfonylethanol, revealed interesting features as a temporary 3'-phosphate protecting group.
- Felder, Eduard,Schwyzer, Robert,Charubala, Ramamurthy,Pfleiderer, Wolfgang,Schulz, Bernd
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p. 3967 - 3970
(2007/10/02)
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