AI Article Synopsis
- Researchers developed a method for creating optically active tetrahydroquinolines using a gold(I)/Brønsted acid system that combines aminobenzaldehydes or aminophenones with alkynes in one-step reactions.
- This new approach allows for efficient synthesis of compounds with varying chiral centers and functional groups, achieving good to excellent yields while maintaining high selectivity in terms of regio-, diastereo-, and enantioselectivity.
- Initial studies indicate that the stereochemistry of these compounds may influence their biological activity, highlighting their potential for use in drug discovery.
Article Abstract
One-pot sequential asymmetric reactions of aminobenzaldehydes or aminophenones with alkynes catalysed by a gold(I)/Brønsted acid cooperative system are reported. This process provides a highly efficient method for the synthesis of optically active tetrahydroquinolines, with one or two chiral centres at different positions as well as highly divergent functional groups, in good to excellent yields and with high regio-, diastereo- and enantioselectivities. A preliminary study on the effect of stereochemistry on biological activity suggests a potential application of these optically active tetrahydroquinolines in drug discovery processes.
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| http://dx.doi.org/10.1039/c2ob25753j | DOI Listing |
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