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1-(4-AMINO-2-METHOXYPHENYL)PYRROLIDIN-2-ONE synthesis

1synthesis methods
-

Yield:-

Reaction Conditions:

in tetrahydrofuran at 20; for 12 h;

Steps:


Piperazine (3.0 equivalents) was added to a solution of the chloromethyl quinazolinone (1 equivalent) in THF (0.2 M) and the resulting mixture was stirred at room temperature for 12 hours. The reaction mixture was then concentrated under reduce pressure. Silica gel column chromatography (DCM +0.5% NEt3/MeOH=100/0 to 80/20) afforded the corresponding piperazine quinazolinone which was immediately used for the next step.

References:

THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK;Stockwell, Brent R.;Yang, Wan Seok;Larraufie, Marie-Helene US2016/332974, 2016, A1 Location in patent:Paragraph 0208