Much Improved Conditions for the Negishi Cross-Coupling of Iodoalanine Derived Zinc Reagents with Aryl Halides

作者:Ross Andrew J; Lang Hannah L; Jackson Richard F W*
来源:Journal of Organic Chemistry, 2010, 75(1): 245-248.
DOI:10.1021/jo902238n

摘要

A combination of Pd(2)(dba)(3) and SPhos (1:2 molar ratio) is an excellent precatalyst for the Negishi cross-coupling of the serine-derived organozinc reagent 2 with aryl halides, including previously difficult ortho-substituted examples. In the case of meta- and para-substituted aryl halides, Pd-loadings of 0.5 mol % give satisfactory results. Use of 2-iodoaniline as substrate gives the lactam 12 in good yield.

  • 出版日期2010-1-1