4-((3-ethynyl-4-fluorophenyl)amino)-7-methoxyquinazolin-6-ol synthesis

12synthesis methods

Product Name:4-((3-ethynyl-4-fluorophenyl)amino)-7-methoxyquinazolin-6-ol
CAS Number:1012057-64-5
Molecular formula:C17H12FN3O2
Molecular Weight:309.29

4-((3-ethynyl-4-fluorophenyl)amino)-7-methoxyquinazolin-6-yl acetate

1012057-63-4
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4-((3-ethynyl-4-fluorophenyl)amino)-7-methoxyquinazolin-6-ol

1012057-64-5
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Yield:1012057-64-5 100%

Reaction Conditions:

Stage #1: 4-((3-ethynyl-4-fluorophenyl)amino)-7-methoxyquinazolin-6-yl acetatewith lithium hydroxide;water in methanol at 20; for 0.5 h;
Stage #2: with acetic acid in methanol;water;

Steps:

31.31f

A mixture of compound 0606 (260 mg, 0.74 mmol), LiOH H₂O (250 mg, 5.8 mmol) in methanol (25 ml) and H₂O (25 ml) was stirred at room temperature for 0.5 hour. The mixture was neutralized by addition of dilution acetic acid. The precipitate was isolated and dried to give the title compound 0607 (234 mg, 100%) as a grey solid: LCMS: 310[M+l]⁺.

References:

WO2008/33747,2008,A2 Location in patent:Page/Page column 140

1072-85-1 Synthesis