反应详情

A mixture of 484 mg (1.3 mmol) of 2-[[3-(2-amino-2-oxoethyl)-2-methyl-1-(phenylmethyl)-1H-indol-4-yl]oxy]acetic acid methyl ester (Example 39) and 2 mL of hydrazine in 10 mL of ethanol was heated to maintain reflux for 16 hours, 10 mL of ethanol added, heated an additional 4 hours and cooled. Ethyl acetate and water were added and the insoluble material filtered. The ethyl acetate solution was separated, washed with brine, dried (MgSO4) and concentrated. The residue was combined with he precipitate above co give 435 mg (91% yield) of 4-(2-hydrazino-2-oxoethoxy)-2-methyl-1-(phenylmethyl)-1H-indole-3-acetamide, mp, 207-210° C.

1. temperaturewas heated
2. temperatureto maintain
3. temperaturereflux for 16 hours
4. temperatureheated an additional 4 hours
5. temperaturecooled
6. filtrationthe insoluble material filtered
7. customThe ethyl acetate solution was separated
8. washwashed with brine
9. dry with materialdried (MgSO4)
10. concentrationconcentrated
11. customprecipitate above co