Diisopropylethylamine → HCID 71667528, compound

Participants

Reaction Steps

2-Cyclopropyl-oxazole-4-carboxylic acid 1h (74.8 mg, 0.489 mmol) was taken in DMF (5.0 ml) and HATU (212.3 mg, 0.558 mmol) was added to this and stirred for 3 min. N,N-diisopropylethylamine (0.243 mL, 1.396 mmol) was added to this and the mixture was stirred again for 3 min. 5-Amino-2-methoxy-N-[3-(2-oxo-pyrrolidin-1-yl)-propyl]-4-(4-o-tolyl-piperazin-1-yl)-benzamide 2b (130.0 mg, 0.279 mmol) was added and the reaction mixture was stirred at room temperature for 16 h. A saturated solution of lithium chloride was added and the product was extracted with ethyl acetate. Organic layer was washed with brine and dried over anhydrous sodium sulfate and concentrated to give the crude product 2c which was purified on preparative HPLC using water/methanol as eluent.

Provenance & Evidence