Stereo- and Regiocontrolled Methylboration of Terminal Alkynes

末端炔烃的立体选择性和区域选择性甲基硼化反应

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Abstract

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.

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