8-bromo-5-fluoroisoquinolin-3-amine synthesis

3synthesis methods

Product Name:8-bromo-5-fluoroisoquinolin-3-amine
CAS Number:1221974-48-6
Molecular formula:C9H6BrFN2
Molecular Weight:241.06

Ethanimidamide, N-[(2-bromo-5-fluorophenyl)methyl]-2,2-diethoxy-

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1221974-48-6
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Yield:1221974-48-6 40.6%

Reaction Conditions:

with sulfuric acid in dichloromethane at 80; for 16 h;

Steps:

346.D Step D: 8-bromo-5-fluoroisoquinolin-3-amine

To a mixture of N-(2-bromo-5-fluorobenzyl)-2,2-diethoxyacetimidamide(1.6 g, 4.80 mmol) and dichloromethane (2 mL) was added H2SO4 (1.280 ml., 24.01mmol). The reaction mixture was stirred at 80° C. for 16 hours, cooled to rt., diluted with EtOAc (100 ml.), quenchedwith ice-water, and neutralized with NaHC03 solution. Theorganic phase was washed with water, dried over Na2S04 ,and evaporated. The residue was purified on an 80 g Thompsonsilica cartridge (3% to 100% EtOAc in Hexanes, 1200mL). The desired product was obtained as a pale yellow solid(0.47 g, 1.950 mmol, 40.6% yield).

References:

JP5714745,2015,B2 Location in patent:Paragraph 0715; 0719

747392-34-3 Synthesis

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References

57381-39-2 Synthesis

57381-39-2
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References