Dimethyl-p-toluidine → 2-Chloro-4-(2,4-dimethoxy-benzyl)-7-isopropyl-3,4-dihydro-benzo[e][1,4]diazepin-5-one

Participants

Reaction Conditions

Reaction Steps

4-(2,4-Dimethoxy-benzyl)-7-isopropyl-3,4-dihydro-1H-benzo[e][1,4]diazepine-2,5-dione (1.5 g, 4.1 mmol) and N,N-dimethyl-p-toluidine (1.76 mL, 12.2 mmol) were mixed in toluene (8 mL) and heated to 100° C. Then phosphorus oxychloride (559 μL, 6.1 mmol) was added dropwise and heating at 100° C. was continued for 2.5 h. After cooling, the mixture was evaporated and dissolved in THF (10 mL) and was used directly in the subsequent step.

Provenance & Evidence