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Ethyl 2-(4-oxo-3,4-dihydroquinazolin-2-yl)acetate synthesis

9synthesis methods
-

Yield:21419-63-6 69.4%

Reaction Conditions:

with toluene-4-sulfonic acid in toluene at 90; for 1 h;

Steps:

602.1

(1) Synthesis of intermediate (Pig6-6b) To a solution of 67.5 parts of toluene in 13 parts of ethyl 3,3-diethoxyacrylate were added 6.8 parts of o-aminobenzamide and 0.1 parts of p-toluenesulfonic acid, followed by heating at 90°C, and stirring for 1 hour while distilling off low-boiling components from the reaction system. After the reaction was complete, the reaction solution was cooled to room temperature, and the precipitated crystals were separated by filtration and washed with hexane to obtain 8.0 parts (yield: 69.4%) of an intermediate (Pig-6b). 1H-NMR(CDCl3): 10.90(s br, 1H), 8.28(d, 2H), 7.75(m, 1H), 7.66(m, 1H), 7.48(m, 1H), 4.26(q, 2H), 1.31(t, 3H)

References:

EP2264105,2010,A1 Location in patent:Page/Page column 173-174