تفاعل #49519

معادلة التفاعل

4-chloro-3-hydroxy-5-fluoro-2-(1-methyl-1-phenylethyl)isoindolinone

TMEDA

iodine

→

3-hydroxy-4-chloro-5-fluoro-7-iodo-2-(1-methyl-1-phenylethyl)isoindolinone

المردود 50.0%

المذيبات

THF

ظروف التفاعل

المعالجة

1. 1
   أخرىfollowed by purification by flash column chromatography (hexane/ethyl acetate=80/20 to 70/30)

الإجراء التجريبي

In a similar manner to Step 3 of Example 16, 4-chloro-3-hydroxy-5-fluoro-2-(1-methyl-1-phenylethyl)isoindolinone (1.20 g, 3.75 mmol) was dissolved in THF (48 mL), and the solution was treated with TMEDA (2.30 mL, 15.0 mmol), sec-butyl lithium-hexane solution (1.01 mol/L, 15.0 mL, 15.0 mmol) and iodine (1.430 g, 5.63 mmol), followed by purification by flash column chromatography (hexane/ethyl acetate=80/20 to 70/30) to obtain 3-hydroxy-4-chloro-5-fluoro-7-iodo-2-(1-methyl-1-phenylethyl)isoindolinone (830 mg, yield 50%).

المصدر