23009-97-4Relevant articles and documents
Solid-Phase Synthesis of 4-Arylazetidin-2-ones via Suzuki and Heck Cross-Coupling Reactions
Ruhland, Beatrice,Bombrun, Agnes,Gallop, Mark A.
, p. 7820 - 7826 (1997)
Application of the Suzuki and the Heck cross-coupling reactions for efficient synthesis of diverse biaryl- and styryl-substituted β-lactams on solid support using an optimized catalyst system is reported. The coupling of phenylboronic acid with the resin-bound 3-phenoxy-4-iodophenyl β-lactam 1a proceeded in 89% isolated yield by employing 20 mol % of the bidentate phosphine-palladium complex, [1,1′-bis(diphenylphosphino)ferrocene]palladium(II) dichloride {PdCl2(dppf)} as catalyst in the presence of triethylamine (TEA, 10 equiv) in DMF at 65 °C for 12 h. Efficient cross-coupling of the iodophenyl β-lactam to heterocyclic boronates and aryl boronates substituted with various electron-donating and -withdrawing groups is also demonstrated. The reverse coupling reactions of immobilized arylboronic acid le with a variety of substituted aryl iodides were found to proceed in excellent yields using the same catalyst system in a 3/7 mixture (v/v) of H2O:DMF at 40 °C. The use of this catalyst for the vinylation of aryl iodide la via the Heck reaction was also examined.
Fragment-based drug design targeting syntenin PDZ2 domain involved in exosomal release and tumour spread
Garcia, Manon,Hoffer, Laurent,Leblanc, Rapha?l,Benmansour, Fatiha,Feracci, Mikael,Derviaux, Carine,Egea-Jimenez, Antonio Luis,Roche, Philippe,Zimmermann, Pascale,Morelli, Xavier,Barral, Karine
, (2021/07/09)
Syntenin stimulates exosome production and its expression is upregulated in many cancers and implicated in the spread of metastatic tumor. These effects are supported by syntenin PDZ domains interacting with syndecans. We therefore aimed to develop, throu
PROCESS FOR THE SEPARATION OF RACEMIC MIXTURES
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Page 6, (2008/06/13)
The present invention relates to a process for the separation of racemic mixtures comprising development of a denser molecular imprint on silica with a desired enantiomer by sol-gel-protocol comprising hydrolytic control polymerization of a silica source as the monomer and amino alkylsilane as a functional monomer in the presence of the desired enantiomer, capping of surface OH groups and desorption of ancapsulated enantiomer from the silica.
Synthesis of metallo-β-lactamase inhibitors
Walter, Magnus W.,Adlington, Robert M.,Baldwin, Jack E.,Schofield, Christopher J.
, p. 7275 - 7290 (2007/10/03)
α-Amido trifluoromethyl alcohols and ketones were synthesised via two independent routes using the Ruppert Reagent (TMS-CF3) and shown to be inhibitors of metallo-β-lactamases.
Trifluoromethyl alcohol and ketone inhibitors of metallo-β-lactamases
Walter, Magnus W.,Felici, Antonio,Galleni, Moreno,Soto, Raquel Paul,Adlington, Robert M.,Baldwin, Jack E.,Frere, Jean-Marie,Gololobov, Mikhail,Schofield, Christopher J.
, p. 2455 - 2458 (2007/10/03)
α-Amido trifluoromethyl alcohols and ketones were synthesised via two independent routes using Ruppert's Reagent (TMS-CF3) and shown to be the first reported synthetic inhibitors of metallo-β-lactamases.