Methyl iodide → HCID 59323262, compound

Participants

Reaction Steps

8.7 mg of tert-butyl 3-(2-propyl sulfonylamino)benzyl-[2-[6-fluoro-3-(4-fluorobenzyl)-3,4-dihydroisoquinolin-2(1H)-yl]ethyl]carbamate obtained in Example 131-a) was dissolved in 1 mL of THF, and 0.7 mg of sodium hydride was added thereto under ice-cooling, followed by stirring for 15 minutes. 2.6 mg of iodomethane was added thereto, followed by stirring at room temperature for 3 hours. After completion of the reaction, the reaction liquid was under ice-cooling, and a saturated aqueous sodium bicarbonate solution and ethyl acetate were added thereto. The organic layer was separated, the aqueous layer was further extracted by addition of ethyl acetate, and the organic layer was combined and washed with saturated brine. The organic layer was dried over anhydrous sodium sulfate and then concentrated under reduced pressure, and the solvent was removed by evaporation to obtain 10.0 mg of a crude composition. The crude composition was purified by PLC to obtain 6.3 mg (yield 71%) of a desired product.

Provenance & Evidence