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Benzeneacetic acid, 4-(1,3-dihydro-1-oxo-2H-isoindol-2-yl)-α-ethyl-, ethyl ester synthesis

10synthesis methods
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Yield:36691-02-8 41.7%

Reaction Conditions:

with copper (I) iodide;N1-benzyl-N2-(2-methylnaphthalen-1-yl)oxalamide;potassium carbonate in N,N-dimethyl-formamide at 120;Reagent/catalyst;

Steps:

2-28 Example 2

Take a 2ml vial, add anhydrous K2CO3 (13.82mg, 0.1mmol, 2.00equiv), dissolve 283mg of ethyl 2-(4-chlorophenyl)butyrate and 199.75mg of isoindolin-1-one in 10ml of DMF ,0.4ml were taken into 2ml vials, each containing ethyl 2-(4-chlorophenyl)butyrate (11.32mg, 0.05mmol, 1.00equiv) and isoindolin-1-one (7.99mg, 0.06mmol, 1.2equiv), take CuI (0.95mg, 0.005mmol, 0.1equiv) and ligand (0.005mmol, 0.1equiv) were added to 0.1ml DMF bottle, respectively, after stirring and complexing for 10min, added to the above 25 vials, After marking, the reaction was stirred at 120° C. overnight. The reaction solution was analyzed by high performance liquid chromatography (HPLC), and 41.7% of the product was produced.

References:

CN114605305,2022,A Location in patent:Paragraph 0030-0084

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