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99512-70-6

4-Methyl-quinazolin-8-ol synthesis

4synthesis methods
4502-10-7 Synthesis
2'-AMINO-3'-HYDROXYACETOPHENONE

4502-10-7
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$18.00/1g

formamide

60100-09-6
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4-Methyl-quinazolin-8-ol

99512-70-6
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Yield:99512-70-6 90%

Reaction Conditions:

at 180; for 0.75 h;Microwave irradiation;

Steps:

11.i Example 11 Preparation of (S)-N-methyl-8-(1-((6-(6-methylpyridin-3-yl)pyrimidin-4-yl)amino)propan-2-yl)quinazoline-4-carboxamide (Compound 971)

As shown in step 11-i of Scheme 11, 1-(2-amino-3-hydroxyphenyl)ethanone (4.0 g, 26.5 mmol) and formamide (20 mL, 45 mmol) were heated at 180° C. under microwave irradiation for 45 minutes.
After cooling, water was added and the reaction mixture concentrated under reduced pressure.
The residue was purified by medium pressure silica gel chromatography (2% MeOH/DCM) to produce 4-methylquinazolin-8-ol (compound 2046, 3.81 g, 90% yield) as a yellow solid.
This product was used as is in subsequent reactions.

References:

US2013/281431,2013,A1 Location in patent:Paragraph 0285