To demonstrate the usefulness of this reaction, application to the gram scale and diversification were conducted (Figure ). We tried to diversify the compound and scale up this reaction using lithocholic acid methyl ester (94), which contains the Relyvrio TM scaffold in its molecule. As expected, the reaction proceeded well at the 10 mmol scale (3.9 g of 94) and the target compound 95 was successfully obtained in 60% yield (dr = 1:1, 2.9 g). Further attempts were made to diversify 94 on the 0.4 mmol scale. It was found that various Michael acceptors could be introduced into 94 in a single step (96-105). This diversification method could be applied to various bioactive and medically important compounds with hydroxyl groups.