反应详情

A 1 molar solution of potassium t-butoxide (0.57 mL, 0.57 mmol) was added to a -78° C. suspension of the phosphonium salt (0.290 g, 0.55 mmol) of Step 4, in 3 mL of THF. The temperature was brought to 0° C. for 20 min then lowered back to -78° C. followed by the addition of a 0.5 molar solution of methyl 1-(((1(R)-(3-formylphenyl)3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio)methyl)cyclopropaneacetate (1.47 mL, 0.44 mmol) of Step 17 of Example 1. The bath was brought to 0° C. for 1 hr and the reaction mixture was quenched with a 25% aqueous NH4OAc. The organic solvents were evaporated and the title product was purified by flash chromatography on silica with EtOAc:hexane 30:70 to yield 0.270 g (94%).

1. customthen lowered back to -78° C.
2. waitThe bath was brought to 0° C. for 1 hr
3. customthe reaction mixture was quenched with a 25% aqueous NH4OAc
4. customThe organic solvents were evaporated
5. customthe title product was purified by flash chromatography on silica with EtOAc:hexane 30:70
6. customto yield 0.270 g (94%)