- Direct release of nitriles from solid phase
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Cleavage conditions are described which allow resin bound secondary amides to be liberated from Sieber or Rink resin as nitriles. The method has been applied to the synthesis of a series of cyanobiaryls. Published by 2001 Elsevier Science Ltd.
- Hone, Neal D.,Payne, Lloyd J.,Tice, Colin M.
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- Synthesis of functionally substituted unsymmetrical biaryls via a novel double metal catalyzed coupling reaction
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Unsymmetrical biaryls containing 'reactive' functional groups (e.g., nitrile or ester groups) can be synthesized in an efficient manner by the direct Ni- or Pd-catalyzed coupling of aryl halides (X = Cl, Br, I) with aryl Grignard (or -lithium) reagents, provided that a catalytic amount of a Zn or Cd salt is also present.
- Miller, Joseph A.,Farrell, Robert P.
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- A General Strategy for Site-Selective Incorporation of Deuterium and Tritium into Pyridines, Diazines, and Pharmaceuticals
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Methods to incorporate deuterium and tritium atoms into organic molecules are valuable for medicinal chemistry. The prevalence of pyridines and diazines in pharmaceuticals means that new ways to label these heterocycles will present opportunities in drug design and facilitate absorption, distribution, metabolism, and excretion (ADME) studies. A broadly applicable protocol is presented wherein pyridines, diazines, and pharmaceuticals are converted into heterocyclic phosphonium salts and then isotopically labeled. The isotopes are incorporated in high yields and, in general, with exclusive regioselectivity.
- Koniarczyk, J. Luke,Hesk, David,Overgard, Alix,Davies, Ian W.,McNally, Andrew
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(2018/02/19)
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