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2-(4-BENZYL-MORPHOLIN-2-YLMETHYL)-ISOINDOLE-1,3-DIONE synthesis

2synthesis methods
-

Yield:110859-48-8 90.6%

Reaction Conditions:

with potassium carbonate in N,N-dimethyl-formamide at 120;

Steps:

15.1

Into a 50mL-1-neck-rbf, 4-benzyl-2-(chloromethyl)morpholine (1 g, 4.43 mmol) and potassium phthalimide (1.65 g, 8.91 mmol) were charged, and were dissolved in dimethylformamide(3ml). K2CO3(1.23 g, 8.90 mmol) was charged thereto, and the mixture was heated to 120, followed by stirring overnight. After the completion of the reaction was monitored with TLC, the resultant product was cooled to room temperature, and slowly added with water (3 ml) to produce a solid. The product was stirred for 1 hour, and filtered. The produced solid was washed with water, and dried in a 60 oven so as to provide 2-(4-benzylmorpholine-2-yl)methylphthalimide (1.35 g, 90.6 %). The dried mixture was directly used in the following reaction

References:

WO2012/128582,2012,A2 Location in patent:Page/Page column 109