Branched allylic sulfones are privileged scaffolds widely distributed in bioactive molecules, and organic functional materials. Some methods for the synthesis of allyl sulfones have been developed, such as Tsuji-Prost reaction, hydrosulfonylation and radical addition reactions. Despite these advances, the transition-metal-free hydrosulfonylation of unactive 1,3-diene leading to branched allylic sulfones has rarely explored.Herein, a boron-catalysed highly regioselective hydrosulfonylation of 1,3-diene with sul nic acid has been explored to construct a broad scope of branched allylic sulfones. The reactions proceed smoothly without the help of transition-metal-catalyst. Abundant structural motifs have also been obtained through simple transformation from the generated allylic sulfone products.Compared with the previous methods, this protocol exhibited advantages as following: 1) readily available starting material without pre-treatment; 2) under the catalysis of inexpensive boron tri uoride etherate, avoidance of transition-metal-catalyst; 3) simple operation and easy scale-up, and does not require dry conditions, an inert atmosphere or a water scavenger; 4) excellent atom economy and regioselectivity.

B(C6F5)3-catalyzed cross-coupling reaction between allylic alcohols and boronic acids with excellent regioselectivity, broad scope and mild conditions.

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Branched allylic sulfones are privileged scaffolds widely distributed in bioactive molecules, and organic functional materials. Some methods for the synthesis of allyl sulfones have been developed, such as Tsuji-Prost reaction, hydrosulfonylation and radical addition reactions. Despite these advances, the transition-metal-free hydrosulfonylation of unactive 1,3-diene leading to branched allylic sulfones has rarely explored. Herein, a boron-catalysed highly regioselective hydrosulfonylation of 1,3-diene with sulfinic acid has been explored to construct a broad scope of branched allylic sulfones. The reactions proceed smoothly without the help of transition-metal-catalyst. Abundant structural motifs have also been obtained through simple transformation from the generated allylic sulfone products. Compared with the previous methods, this protocol exhibited advantages as following: 1) readily available starting material without pre-treatment; 2) under the catalysis of inexpensive boron trifluoride etherate, avoidance of transition-metal-catalyst; 3) simple operation and easy scale-up, and does not require dry conditions, an inert atmosphere or a water scavenger; 4) excellent atom economy and regioselectivity.

The exploration of novel green synthetic strategies to obtain useful organic molecules is one of the most important missions for sustainable development. Herein, an efficient and sustainable decarboxylative oxysulfonylation between arylpropiolic acids and sodium sulfinates has been established, providing a broad scope of β-ketosulfones in excellent yields. The reactions proceed at room temperature employing air as the only oxidant and oxygen source without extra catalyst, oxidant, and additive. Additionally, the reaction is scalable, and the products have been easily isolated by simple recrystallization, avoiding the chromatographic purification. Mechanistic studies have also been conducted to reveal that the reaction proceed via a radical mechanism.