反应详情

The compound of step 2 (0.410 g, 1.22 mmol) was dissolved in DMF (5 ml), EDIA (0.790 g, 6.12 mmol), HOBT (33 mg, 0.244 mmol), and 2-amino-indane-2-carboxylic acid methyl ester hydrochloride (0.246 g, 1.47 mmol) were added, the mixture was cooled in an ice bath and EDC (352 mg, 1.84 mmol) was added. The mixture was stirred overnight. The volatiles were evaporated in vacuo, the mixture was partitioned between 2 N hydrochloric acid and EA, the organic phase was dried over magnesium sulfate and evaporated to dryness. The residue was purified by silica gel chromatography (HEP/EA gradient) to give 0.56 g of the title compound.

1. temperaturethe mixture was cooled in an ice bath
2. customThe volatiles were evaporated in vacuo
3. customthe mixture was partitioned between 2 N hydrochloric acid and EA
4. dry with materialthe organic phase was dried over magnesium sulfate
5. customevaporated to dryness
6. customThe residue was purified by silica gel chromatography (HEP/EA gradient)