1-chloro-5-fluoroisoquinoline synthesis

Yield:-

Reaction Conditions:

with trichlorophosphate at 80; for 2 h;

Steps:

1.1 Step 1. Synthesis of 1-chloro-5-fluoroisoquinoline

Add 5-fluoroisoquinolin-1(2H)-one (450mg) to phosphorus oxychloride (8mL),The reaction system was then stirred at 80°C for 2 hours.After the reaction was completed, the solvent was concentrated, the reaction residue was dissolved in dichloromethane and washed with saturated sodium bicarbonate solution, the organic phase was washed with saturated brine, dried over anhydrous sodium sulfate, and filtered,Concentrate to remove the solvent to obtain 1-chloro-5-fluoroisoquinoline as a white solid compound (480mg, yield 96%),The product can be used directly in the next step without purification;

References:

CN111138355,2020,A Location in patent:Paragraph 0080-0082