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Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
Mg/CH3OD-Mediated Multideuteration of 2-Vinylquinolines and 2-Methylquinolines
Peng-Hui Ma1, Peng Zhou1, Zhong-Xu Pei1
1College of Pharmacy, Nankai University, Tianjin300353, P. R. China.
Abstract:
Herein, we report a convenient and efficient method for the reductive multideuteration of 2-vinylquinolines and 2-methylquinolines utilizing a Mg/CH3OD system. By employing readily available CH3OD as a deuterium source, this method achieves 3-5 deuterium atoms incorporation into the target structures. Moreover, the Mg/CH3OH system smoothly reduced quinoline substrates to the corresponding tetrahydroquinoline products. This protocol offers a practical and mild approach for high-level deuterium incorporation using inexpensive reagents while avoiding complex catalysts and harsh conditions. This work opens up a new avenue for the use of Mg/CH3OD in deuterium labeling.
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