- OXAZOLIDINONE HYDROXAMIC ACID COMPOUNDS FOR THE TREATMENT OF BACTERIAL INFECTIONS
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This invention pertains generally to treating bacterial infections using organic compounds of Formula I. In certain aspects, the invention pertains to treating infections caused by Gram-negative bacteria. (I) wherein X, Y, R1, R2, R3, R4 and R5 and defined herein.
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Page/Page column 96
(2015/05/19)
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- Practical synthesis of aryl-2-methyl-3-butyn-2-ols from aryl bromides via conventional and decarboxylative copper-free Sonogashira coupling reactions
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Two efficient protocols for the palladium-catalyzed synthesis of aryl-2-methyl-3-butyn-2-ols from aryl bromides in the absence of copper were developed. A simple catalytic system consisting of Pd(OAc)2 and P(p-tol)3 using DBU as the base and THF as the solvent was found to be highly effective for the coupling reaction of 2-methyl-3-butyn-2-ol (4) with a wide range of aryl bromides in good to excellent yields. Analogously, the synthesis of aryl-2-methyl-3-butyn-2-ols was performed also through the decarboxylative coupling reaction of 4-hydroxy-4-methyl-2-pentynoic acid with aryl bromides, using a catalyst containing Pd(OAc)2 in combination with SPhos or XPhos in the presence of tetra-n-butylammonium fluoride (TBAF) as the base and THF as the solvent. Therefore, new efficient approaches to the synthesis of terminal acetylenes from widely available aryl bromides rather than expensive iodides and using 4 or propiolic acid rather than TMS-acetylene as inexpensive alkyne sources are described.
- Caporale, Andrea,Tartaggia, Stefano,Castellin, Andrea,De Lucchi, Ottorino
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supporting information
p. 384 - 393
(2014/03/21)
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- LITHIUM PEROXYACETYLENIDES IN THE SYNTHESIS OF PEROXYALKYNOIC ACIDS
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A method was proposed for synthesizing 4-methyl-4-tert-alkyl(cycloalkyl, aralkyl)peroxy-2-pentynoic acids by metallation of appropriate monosubstituted peroxyalkynes with butyllithium followed by carboxylation of the initially formed lithium peroxyacetylenides with solid carbon dioxide.Cyclohexylammonium salts of the peroxyalkynoic acids synthesized were prepared.
- Yuvchenko, A.P.,Dikusar, E.A.,Zhukovskaya, N.A.,Moiseichuk, K.L.
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p. 2146 - 2151
(2007/10/02)
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