Triphenylphosphine → methyl 4-{[(6-{(2-fluoropropyl)[(4-methyl-1,3-thiazol-2-yl)sulfonyl]amino}-2,3-dihydro-1H-inden-5-yl)oxy]methyl}benzoate

Participants

Reaction Steps

311 mg of methyl 4-{[(6-{[(4-methyl-1,3-thiazol-2-yl)sulfonyl]amino}-2,3-dihydro-1H-inden-5-yl)oxy]methyl}benzoate, 63.6 mg of 2-fluoro-1-propanol, and 356 mg of triphenylphosphine were dissolved in 4.0 mL of THF, and 591 mg of diethyl azodicarboxylate was added thereto under ice-cooling, followed by stirring at room temperature for 20 hours. The reaction liquid was concentrated under reduced pressure and the obtained residue was purified by silica gel column chromatography (hexane:ethyl acetate=100:0 to 60:40) to obtain 364 mg of methyl 4-{[(6-{(2-fluoropropyl)[(4-methyl-1,3-thiazol-2-yl)sulfonyl]amino}-2,3-dihydro-1H-inden-5-yl)oxy]methyl}benzoate.

Provenance & Evidence