تفاعل #66723

معادلة التفاعل

ethyl acetate

7-Chloro-6-fluoro-2H-isoquinolin-1-one

benzyl bromide

benzyl bromide

→

title compound 1

1-Benzyloxy-7-chloro-6-fluoro-isoquinoline

المذيبات

THF

ظروف التفاعل

المعالجة

1. 1
   workup.STIRRINGthe mixture was stirred at 70° C. for 2 h
2. 2
   درجة الحرارةAfter cooling down to room temperature
3. 3
   ترشيحfiltered over celite
4. 4
   غسيلThe filter cake was washed thoroughly
5. 5
   أخرىthe organic layer was evaporated

الإجراء التجريبي

7-Chloro-6-fluoro-2H-isoquinolin-1-one (prepared according to WO 2007/012422; 52.2 g) was dissolved in THF (1 L). After addition of silver carbonate (145.5 g) and benzyl bromide (40.6 mL), the mixture was stirred at room temperature overnight. Another 6.2 mL of benzyl bromide were added and the mixture was stirred at 70° C. for 2 h. After cooling down to room temperature, the reaction mixture was diluted by addition of 1 L of ethyl acetate and filtered over celite. The filter cake was washed thoroughly, the organic layer was evaporated and subjected to silica gel chromatography (n-heptanes: methyl tert. butyl ether) to give 27.8 g of the title compound 1. Rt=3.73 min (Method 1). Detected mass: 288.1 (M+H+).

المصدر