摘要
A series of proline-based amino pyridine dipeptide organocatalysts was synthesized and applied in direct asymmetric intermolecular aldol reaction. These catalysts showed good solubility in organic solvents, good yields （73%--97%） and enantioselectivitives（74%--94%）. Among them, dipeptide organocatalyst（2） was found to be the most efficient one for the asymmetric aldol reaction between cyclohexanone and 4-nitrobeznaldehyde. After optimizing the catalytic reaction conditions, we found that the catalyst showed high yield（97%）, enantioselectivity（e.e., up to 92%） and anti-diastcreoselectivity（up to 95：5） at mild room temperature without any additives.
A series of proline-based amino pyridine dipeptide organocatalysts was synthesized and applied in direct asymmetric intermolecular aldol reaction. These catalysts showed good solubility in organic solvents, good yields （73%--97%） and enantioselectivitives（74%--94%）. Among them, dipeptide organocatalyst（2） was found to be the most efficient one for the asymmetric aldol reaction between cyclohexanone and 4-nitrobeznaldehyde. After optimizing the catalytic reaction conditions, we found that the catalyst showed high yield（97%）, enantioselectivity（e.e., up to 92%） and anti-diastcreoselectivity（up to 95：5） at mild room temperature without any additives.
基金
Supported by the National Natural Science Foundation of China(Nos.20802025 and 20082011)
