Key Laboratory for Advanced Materials and Institute of Fine Chemicals, East China University of Science and Technology , Shanghai 200237, PR China.
J Org Chem. 2014 May 16;79(10):4332-9. doi: 10.1021/jo500145w. Epub 2014 May 5.
The first organocatalytic enantioselective Mannich reaction of pyrazoleamides with isatin-derived N-Boc ketimines has been developed to afford 2-oxindole-based chiral β-amino amides in good yields (84-97%) with excellent diastereo- and enantioselectivities (up to 99:1 dr and >99% ee).
已开发出首例吡唑酰胺与色胺衍生的 N-Boc 酮亚胺的手性有机催化对映选择性曼尼希反应,以高产率(84-97%)和优异的非对映选择性和对映选择性(高达 99:1 dr 和>99%ee)获得基于 2-氧吲哚的手性β-氨基酰胺。