State Key Laboratory of Applied Organic Chemistry, College of Chemistry and Chemical Engineering, Lanzhou University, Lanzhou 730000, People's Republic of China.
J Org Chem. 2011 Sep 16;76(18):7551-5. doi: 10.1021/jo201123p. Epub 2011 Aug 18.
A highly efficient asymmetric Michael addition of 1-acetylindolin-3-ones to α,β-unsaturated aldehydes is developed to afford 2-substituted indolin-3-one derivatives in high yields (up to 94%) with good stereoselectivities (up to 11:1 dr and 96% ee). The Michael adducts can be transformed into substituted cyclopentyl[b]indoline compounds conveniently without racemization.
发展了一种高效的不对称迈克尔加成反应，用于 1-乙酰基吲哚啉-3-酮与α,β-不饱和醛的加成反应，以高产率（高达 94%）和良好的立体选择性（高达 11:1 dr 和 96%ee）得到 2-取代的吲哚啉-3-酮衍生物。迈克尔加成产物可以方便地转化为取代的环戊基[b]吲哚啉化合物，而不会发生外消旋化。
