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4-HYDROXY-7-CHLORO-3-IODOQUINOLINE synthesis

4synthesis methods
-

Yield:860236-13-1 87%

Reaction Conditions:

with N-iodo-succinimide;acetic acid at 60; for 5 h;

Steps:

3 3) A Compound of Formula (I) Where X═I

N-iodosuccinimide (626 mg, 2.78 mmol) was added to a suspension of 7-chloroquinolin-4-ol (500 mg, 2.78 mmol) in 16 mL of acetic acid. The reaction is heated at 60° C. for 5 hours and then diluted in water and filtered. The white solid is washed with water and dried under vacuum. (0257) Yield 87%. White solid; RMN 1H (DMSO, 400 MHz) δ 7.39 (1H, dd, J=8.8, 2.2 Hz); 7.62 (1H, d, J=2.2 Hz); 8.10 (1H, d, J=8.8 Hz), 8.55 (s, 1H); 12.21 (sl, 1H); RMN 13C (DMSO, 100 MHz) δ 81.3; 117.6; 120.9; 124.4; 127.3; 140.3; 145.3; 172.5. SM (ESI+): m/z=523 [M+1]

References:

US2019/62278,2019,A1 Location in patent:Paragraph 0255-0257