1,2-Dichloroethane → HCID 86690917, compound

Participants

Reaction Steps

54 mg (0.10 mmol) of the compound from Example 60 were initially charged in 4 ml of DMF, and 19 mg (0.13 mmol) of HOBt and 24 mg (0.03 mmol) of EDC were added. After 10 min of stirring at RT, 0.1 ml (1.93 mmol) of ammonia solution (32% strength in water) were added and the mixture was stirred at room temperature for 16 h. The reaction solution was then freed from excess ammonia under reduced pressure, about 3 ml of water were added and the mixture was extracted three times with in each case 5 ml of ethyl acetate. The combined organic phases were dried over magnesium sulfate, filtered and concentrated under reduced pressure. The crude product was purified chromatographically [Method 19]. This gave 27 mg (46% of theory) of the target compound.

Provenance & Evidence