After the absolute structure was determined, lineatin quickly attracted considerable synthetic interests due to its natural occurrence, biological activity, and unique structural features. A few routes describing the total synthesis of lineatin was proposed with yields of 0.5–2%. Recently, a new total synthesis route that adopted a photochemical [2 + 2] cycloaddition approach to construct diastereoselective cyclobutene and a regiocontrolled oxymercuration reaction was proposed. This route achieved in synthesizing highly pure (+)-lineatin (> 99.5% ee) through 14 steps and resulted in 14% overall yield from a homochiral 2(5H)-furanone. (Figure 1 showed the basic outline of this approach).