- HYDROXAMIC ACID DERIVATIVES AS GRAM-NEGATIVE ANTIBACTERIAL AGENTS
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The invention relates to chemical compounds of formula (IB): or a salt thereof. In some embodiments, the invention relates to inhibitors of UDP-3-0 — (R-S-hydroxymyristoyl)-N-acetylglucosamine deacetylase (LpxC). In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein and their use in the prevention and/or treatment of Gram- negative bacterial infections.
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Page/Page column 195
(2010/09/18)
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- Buchwald-Hartwig Mono-N-arylation with 2,6-dihaloisonicotinic acid derivatives: A convenient desymmetrization method
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A method for the Buchwald-Hartwig mono-N-arylation of aniline with methyl 2,6-dichloroisonicotinate using Pd(OAc)2, XPhos, and t-BuONa is reported. Use of m-anisidine under the same conditions resulted in the amidation of the methyl ester. Mono-N-arylation of m-anisidine with 2,6-dichloro-N,N- diisopropylisonicotinamide and 2,6-dibromo-N,N-diisopropylisonicotinamide, however, was successfully achieved using Pd(OAc)2/XPhos/t-BuONa or Pd(OAc)2/(±)-BINAP/K2CO3, respectively. The present study demonstrates the sensitivity of this cross-coupling method to both the steric and electronic nature of the coupling partners. Georg Thieme Verlag Stuttgart.
- Lorimer, Anna V.,O'Connor, Patrick D.,Brimble, Margaret A.
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experimental part
p. 2764 - 2770
(2009/04/07)
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