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  • Iodocyclization, followed by palladium-catalyzed coupling: a versatile strategy for heterocyclic library construction.

Iodocyclization, followed by palladium-catalyzed coupling: a versatile strategy for heterocyclic library construction.

Combinatorial chemistry & high throughput screening (2012-01-26)
Anton V Dubrovskiy, Nataliya A Markina, Richard C Larock
RESUMO

The iodocyclization of functionally-substituted alkynes provides an excellent way to prepare a wide range of iodoheterocycles, which can then be readily elaborated through palladium-catalyzed Suzuki-Miyaura, Sonogashira, Heck, Hartwig-Buchwald, and carbonylation processes into libraries of medicinally relevant heterocycles. The synthesis of libraries of indoles, benzofurans, benzothiophenes, isocoumarins and pyrones, cyclic imidates, isoxazoles, furans using this approach is reviewed. This technology is very versatile, proceeds under mild reaction conditions in high yields, and tolerates considerable functionality.

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Palladium, powder, <1 μm, ≥99.9% trace metals basis
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Palladium black, surface area 40-60 m2/g, 99.95% trace metals basis
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Palladium, foil, thickness 0.025 mm, 99.9% trace metals basis
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Palladium, wire, diam. 0.5 mm, 99.9% trace metals basis
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Palladium, wire, diam. 1.0 mm, 99.9% trace metals basis
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Palladium, foil, thickness 0.05 mm, 99.9% trace metals basis
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Palladium, foil, thickness 0.5 mm, 99.9% trace metals basis
Palladium, foil, 25x25mm, thickness 0.25mm, as rolled, 99.95%
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Palladium, evaporation slug, diam. × L 0.6 cm × 0.6 cm, 99.95% trace metals basis
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Palladium, foil, thickness 0.25 mm, 99.98% trace metals basis
Palladium, foil, 50x50mm, thickness 0.1mm, as rolled, 99.95%
Palladium, foil, light tested, 25x25mm, thickness 0.006mm, 99.95%
Palladium, foil, light tested, 25x25mm, thickness 0.025mm, as rolled, 99.95%
Palladium, foil, light tested, 25x25mm, thickness 0.025mm, as rolled, 99.99+%
Palladium, foil, light tested, 25x25mm, thickness 0.03mm, as rolled, 99.95%
Palladium, foil, light tested, 25x25mm, thickness 0.047mm, as rolled, 99.95%
Palladium, foil, light tested, 25x25mm, thickness 0.075mm, as rolled, 99.95%
Palladium, foil, light tested, 50x50mm, thickness 0.025mm, as rolled, 99.95%
Palladium, foil, light tested, 50x50mm, thickness 0.025mm, as rolled, 99.99+%
Palladium, foil, light tested, 50x50mm, thickness 0.03mm, as rolled, 99.95%
Palladium, foil, light tested, 50x50mm, thickness 0.047mm, as rolled, 99.95%
Palladium, foil, light tested, 50x50mm, thickness 0.075mm, as rolled, 99.95%
Palladium, foil, not light tested, 100x100mm, thickness 0.004mm, 99.95%
Palladium, foil, not light tested, 100x100mm, thickness 0.005mm, 99.95%
Palladium, foil, not light tested, 100x100mm, thickness 0.006mm, 99.95%
Palladium, foil, not light tested, 100x100mm, thickness 0.008mm, 99.95%
Palladium, foil, not light tested, 100x100mm, thickness 0.0125mm, 99.95%

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