反应详情

Alternate Method: Sulfuryl chloride (135 mg, 80.2 μL, 1 mmol) was added at room temperature to a dichloromethane (10 mL) solution of 3-(5-chloro-2-methoxy-phenyl)-3-fluoro-1-methylsulfanylmethyl-6-trifluoromethyl-1,3-dihydro-indol-2-one (420 mg, 1 mmol) in a round-bottomed flask equipped with nitrogen inlet and magnetic stirrer. After stirring the reaction mixture at room temperature for 20 minutes, the crude solution was concentrated in vacuo to afford 3-(5-chloro-2-methoxy-phenyl)-1-chloromethyl-3-fluoro-6-trifluoromethyl-1,3-dihydro-indol-2-one (425 mg, 100% crude yield) as a light yellow solution. Step C: Phosphoric acid mono-[3-(5-chloro-2-methoxy-phenyl)-3-fluoro-2-oxo-6-trifluoromethyl-2,3-dihydro-indol-1-ylmethyl] ester, bis-[tris(hydroxymethyl)ammoniummethane] salt

1. customequipped with nitrogen inlet and magnetic stirrer
2. concentrationthe crude solution was concentrated in vacuo