反应详情

The compound of step 1 (280 mg, 0.885 mmol) was dissolved in DMF (1.3 ml) and HOBT (24 mg), 1-amino-cycloheptanecarboxylic acid methyl ester hydrochloride (221 mg, 1.06 mmol) and EDIA (578 mg, 4.43 mmol) were added. The mixture was cooled in an ice bath and EDC (254 mg, 1.33 mmol) was added. The mixture was stirred at room temperature for 3 days and partitioned between EA and water. The aqueous phase was extracted with EA, the combined organic phases were dried over sodium sulfate and evaporated to dryness. The residue was purified by RP HPLC (water/ACN gradient) to yield the title compound (120 mg).

1. temperatureThe mixture was cooled in an ice bath
2. custompartitioned between EA and water
3. extractionThe aqueous phase was extracted with EA
4. dry with materialthe combined organic phases were dried over sodium sulfate
5. customevaporated to dryness
6. customThe residue was purified by RP HPLC (water/ACN gradient)