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Stereo- and Regiocontrolled Methylboration of Terminal Alkynes

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journal contribution
posted on 09.05.2018, 18:19 by Oleksandr Zhurakovskyi, Rafael M. P. Dias, Adam Noble, Varinder K. Aggarwal
A scalable and operationally simple synthesis of trisubstituted alkenyl boronic esters has been achieved using a Zr-catalyzed carboalumination of terminal alkynes followed by in situ transmetalation with i-PrOBpin. The products are formed in good yields and with excellent regioselectivity and perfect stereoselectivity. The new procedure provides a significant improvement over the previously reported syntheses.