- Cyclization of 5-hexynoic acid to 3-alkoxy-2-cyclohexenones
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The one-pot cyclization of 5-hexynoic acid to produce 3-alkoxy-2- cyclohexenones proceeds in good yields (58-90%). 3-Hexynoic acid was converted to its acyl chloride with the aid of oxalyl chloride and was cyclized to 3-chloro-2-cyclohexenone upon addition of indium(III) chloride. Subsequent addition of alcohol nucleophiles led to the desired 3-alkoxy-2-cyclohexenones.
- Hylden, Anne T.,Uzelac, Eric J.,Ostojic, Zeljko,Wu, Ting-Ting,Sacry, Keely L.,Sacry, Krista L.,Xi, Lin,Jones, T. Nicholas
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experimental part
p. 1323 - 1326
(2011/11/06)
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- Asymmetric allylic alkylation of cyclic vinylogous esters and thioesters by Pd-catalyzed decarboxylation of enol carbonate and β-ketoester substrates
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(Chemical Equation Presented) Excellent yields and enantioselectivities were achieved for the palladium-catalyzed asymmetric allylic alkylation of vinylogous thioesters. The close-to-neutral reaction conditions ensure that this reaction can tolerate a wide range of functionalities. Furthermore, this approach provides a convenient protocol for the synthesis of synthetically important α,α- and γ,γ-di-substituted cycloalkenones.
- Trost, Barry M.,Bream, Robert N.,Xu, Jiayi
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p. 3109 - 3112
(2007/10/03)
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- Indazole compounds and pharmaceutical compositions for inhibiting protein kinases, and methods for their use
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Indazole compounds that modulate and/or inhibit the activity of certain protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating tyrosine kinase signal transduction and thereby modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer and other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, neovascular glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.
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