A quadruple cascade protocol for the one-pot synthesis of fully-substituted hexahydroisoindolinones from simple substrates

• Hong-Bo Zhang,
• Yong-Chun Luo,
• Xiu-Qin Hu,
• Yong-Min Liang and
• Peng-Fei Xu

Beilstein J. Org. Chem. 2016, 12, 253–259, doi:10.3762/bjoc.12.27

• -substituted hexahydroisoindolinones was developed by using bifunctional tertiary amine-thioureas as powerful catalysts. As far as we know, there is no efficient synthetic method developed toward fully-substituted hexahydroisoindolinones. The products were obtained in good yield and diastereoselectivity. The

• one-pot cascade quadruple protocol features readily available starting materials, simple manipulation, mild conditions and good atom economy. Keywords: bifunctional catalysis; hexahydroisoindolinones; one-pot synthesis; quadruple cascade; Introduction Isoindolines and their congeners are one kind of

• is a frontier in organic synthesis. However, compared with the synthesis of their congeners, the synthesis of fully-substituted hexahydroisoindolinones is much more difficult due to the steric hindrance and the high strain of the molecular architectures [17]. Three methods to synthesize 3-substituted