4(3H)-Quinazolinone, 2-amino-8-methoxy- synthesis

Yield:169270-52-4 50 g

Reaction Conditions:

with hydrogenchloride in ethanol;water;Reflux;

Steps:

PI

N-(8-methoxy-4-(lH-l ,2,4-triazol-l-yl)quinazolin-2-yl)acetamide (compound 4)was prepared from a benzoic acid starting material in accordance with Scheme PI by adding into a solution of 2- amino-3-methoxybenzoic acid (compound PI-1) (50 g, 299 mmol) in EtOH (400 ml), cyanamide (18.86 g, 449 mmol) and concentrated HC1 (12 ml, 299 mmol). The reaction mixture thus provided was refluxed overnight and then cooled to room temperature. The precipitates were collected through filtration, washing with cold ethanol to yield compound PI-2 (50 g).

References:

WO2014/101113,2014,A1 Location in patent:Paragraph 0145