7-Fluoro-6-methoxy-quinazolin-4-ol synthesis
- Product Name:7-Fluoro-6-methoxy-quinazolin-4-ol
- CAS Number:869475-52-5
- Molecular formula:C9H7FN2O2
- Molecular Weight:194.16
159768-51-1
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Yield:869475-52-5 83%
Reaction Conditions:
in butan-1-ol at 110; for 2 h;
Steps:
7-fluoro-6-methoxyquinazolin-4-ol:
A mixture of methyl 2-amino-4-fluoro-5- methoxybenzoate (392 mg, 1.97 mmol) and formamidine acetate (205.1 mg, 1.97 mmol) in n- butanol (5 mL) was stirred at 110°C for 2 hours. White solid was precipitated and TLC (Petroleum ether/EtOAc = 5/1) showed the starting material was consumed completely. The mixture was cooled to 25°C and the solid collected by filtration to afford the title compound as a white solid (320 mg, 83%). 1H NMR (500 MHz, DMSO-d6) d: 12.44 (br s, 1H), 8.04 (s, 1H), 7.66 (d, 7=9.5 Hz, 1H), 7.52 (d, 7=12.0 Hz, 1H), 3.96 (s, 3H).
References:
WO2020/163193,2020,A1 Location in patent:Paragraph 00262
159768-51-1
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60100-09-6
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869475-52-5
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159768-50-0
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82846-18-2
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869475-52-5
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74385-37-8
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869475-52-5
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$95.00/100mg