Abstract
1,3-Bis-(boryl)alkanes are useful building blocks in organic synthesis, which enables
a series of functionalizations to build up molecular complexity for the synthesis
of target molecules. However, modular and practical synthesis of such building blocks
remains a challenge. Herein, we report an efficient method for the synthesis of 1,3-diboronates
via Cu-catalyzed borylalkylation of alkenes using iodomethyl boronate as the electrophile.
This reaction provides a wide range of 1,3-bis-(boryl)alkanes in high efficiency under
simple reaction conditions. Notably, this reaction exhibits high modularity, and large-scale
reaction further demonstrated its practicability.
Key words
1,3-diboronates - borylalkylation - Cu catalysis - boron compounds - modular synthesis
