6-bromo-1-chloro-7-methoxyIsoquinoline synthesis
- Product Name:6-bromo-1-chloro-7-methoxyIsoquinoline
- CAS Number:758710-74-6
- Molecular formula:C10H7BrClNO
- Molecular Weight:272.53
758710-73-5
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Yield:758710-74-6 91%
Reaction Conditions:
with trichlorophosphate at 100; for 2 h;Sealed tube;Microwave irradiation;
Steps:
6-Bromo-1-chloro-7-methoxyisoquinoline
6-Bromo-7-methoxyisoquinolin-1(2H)-one (2.06 g, 8.11 mmol) was suspended in phosphorus oxychloride (7.56 mL, 81 mmol) in a sealed 24 mL microwave vial and the mixture heated at 100 °C, forming a dark solution. After 2 hrs the mixture was quenched carefully into lukewarm water (200 mL). The aqueous was taken to pH 7/8 with sat. aq. NaHCO3 solution (250 mL). The aqueous was extracted with EtOAc (3 x 150 mL) and the combined organics washed with brine (100 mL), dried (MgSO4), filtered and concentrated to afford (2.53 g, 91% yield) as an off-white solid after drying under vacuum. [M+H]+ = 272.0/274.0
References:
WO2021/32933,2021,A1 Location in patent:Page/Page column 170
1080-07-5
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