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4-(TRIFLUOROMETHYL)-1,3-DIHYDRO-2H-1,5-BENZODIAZEPIN-2-ONE synthesis

4synthesis methods
-

Yield:2070-87-3 85%

Reaction Conditions:

with L-proline in ethanol at 78; for 4 h;

Steps:

1 Example One:

25ml round bottom flask was addedTrifluoroAcetoacetic acidEthyl ester (184.0mg, 1.0mmol), o-phenylenediamine (108.1 mg, 1.0mmol), 10mLEtOH as solvent, was added L- proline (17.3mg, 0.15mmol), 78 stirred at reflux for 4 hours. TLC plate tracking point, after completion of the reaction, the solvent was rotary evaporated and the residue was purified by column chromatography using petroleum ether: ethyl acetate = 4: 1 (v / v) as eluent, and purified by chromatography to give pure product compound (193.8mg, 85%).

References:

CN105693633,2016,A Location in patent:Paragraph 0024; 0025