反应详情

1.05 g of 1,1-dichloro-3-[1-(2-fluorobenzyl)indazole-3-carboxamido]-pent-1-ene (2.58 mmol) and 5.20 ml of NaOH, 1N (5.20 mmol) were stirred in 15 ml of N-methylpyrrolidone at 50° C. under argon for 2 days. After cooling, the mixture was poured onto ice-water and extracted several times with ethyl acetate. The organic phase was dried (sodium sulphate) and concentrated (N-methylpyrrolidone stripped off under a high vacuum). The residue was purified by column chromatography (aluminium oxide, cyclohexane/ethyl acetate 2:1). 470 mg (52%) of 5-ethyl-2-[1-(2-fluorobenzyl)-indazol-3-yl]-5-hydroxymethyl-oxazole were obtained as white crystals.

1. temperatureAfter cooling
2. additionthe mixture was poured onto ice-water
3. extractionextracted several times with ethyl acetate
4. dry with materialThe organic phase was dried (sodium sulphate)
5. concentrationconcentrated (N-methylpyrrolidone
6. customThe residue was purified by column chromatography (aluminium oxide, cyclohexane/ethyl acetate 2:1)