Iodine → HCID 57826352, compound

Participants

Reaction Steps

Triphenyl phosphine (278 mg, 1.06 mmol), iodine (269 mg, 1.06 mmol) and triethylamine (0.3 mL, 2.12 mmol) were added at 0° C. to a solution in which 7-[2-(4-methoxy-phenyl)-2-oxo-1-pyridin-4-yl-ethylcarbamoyl]-heptanoic acid methyl ester (218 mg, 0.53 mmol) prepared in Step 5 was dissolved in 1.5 mL of methylene chloride, and the resulting mixture was stirred for 30 min. The reaction materials were elevated to room temperature and were further stirred for 1 day. After the reaction was complete, the reaction materials were diluted with 50 mL of ethyl acetate and 50 mL of water to dissolve salts, followed by separation of layers. The obtained organic layer was successively washed twice with 50 mL of a brine solution. The organic layer was dried over magnesium sulfate, filtered, concentrated under reduced pressure and purified by silica gel column chromatography to afford 7-[5-(4-methoxy-phenyl)-4-pyridin-4-yl-oxazol-2-yl)-heptanoic acid methyl ester of the following formula.

Provenance & Evidence