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[摘要]：A method for the Buchwald-Hartwig mono-N-arylation of aniline with 2,6-dichloroisonicotinate using Pd(OAc)2, XPhos, and tBuONa is reported. Use of 3-anisidine under the same conditions resulted in the amidation of the Me ester. Mono-N-arylation of 3-anisidine with 2,6-dichloro- and 2,6-dibromo-N,N-diisopropylisonicotinamide, however, was successfully achieved using Pd(OAc)2/XPhos/tBuONa or Pd(OAc)2/(?-BINAP/K2CO3, resp. The present study demonstrates the sensitivity of this cross-coupling method to both the steric and electronic nature of the coupling partners. |
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