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144783-46-0

1-(4-MORPHOLINO-3-NITROPHENYL)-1-ETHANONE synthesis

4synthesis methods
-

Yield:144783-46-0 88%

Reaction Conditions:

at 90; for 3 h;

Steps:

11 Example 11. Preparations of 2- (5H-imidazo [5, 1-a] isoindol-5-yl) -1- (4-morpholino-3-nitrophenyl) ethanol (Compound 11)

A mixture of 1- (4-fluoro-3-nitrophenyl) ethanone (0.20 g, 1.09 mmol) and morpholine (1.5 mL) was stirred at 90 for 3 h. The reaction mixture was cooled to room temperature, poured to 2 N HCl solution (10 mL) and extracted with EtOAc (10 mL x 3) . The combined organic layers were washed with brine (10 mL) , dried over anhydrous Na2SO4, filtered and concentrated in vacuo to give a residue, which was triturated with a solution of petroleum ether and EtOAc (1 : 1) . The resulting solid was collected by filtration and dried in vacuo to afford compound 11b (0.24 g, 88yield) as a brown solid, which was used for the next step without further purification. MS 251.2 [M+H]+.

References:

WO2016/165613,2016,A1 Location in patent:Paragraph 125

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