Реакция #89410

Уравнение реакции

2-(((2S,3R)-3-methylpiperidin-2-yl)methyl)isoindoline-1,3-dione

5-chloro-2-iodobenzoic acid

DIPEA

HATU

→

title compound

2-(((2S,3R)-1-(5-Chloro-2-iodobenzoyl)-3-methylpiperidin-2-yl)methyl)isoindoline-1,3-dione

Растворители

ethyl acetate

DMF

Условия реакции

Обработка

1. 1
   Промывкаwashed with satd
2. 2
   ДругоеThe organic layer was separated
3. 3
   Сушкаdried with MgSO4
4. 4
   Концентрированиеconcentrated in vacuo
5. 5
   ДругоеThe crude product was purified by chromatography on silica gel (EtOAc/hex)

Методика

A mixture of 2-(((2S,3R)-3-methylpiperidin-2-yl)methyl)isoindoline-1,3-dione (0.70 g, 2.71 mmol), 5-chloro-2-iodobenzoic acid (0.66 g, 2.32 mmol), DIPEA (1.21 mL, 6.97 mmol) and HATU (1.06 g, 2.79 mmol) in DMF (5 ml) was stirred at rt for 1 h. The reaction mixture was diluted with ethyl acetate and washed with satd. aq. NaHCO3 and brine successively. The organic layer was separated, dried with MgSO4 and concentrated in vacuo. The crude product was purified by chromatography on silica gel (EtOAc/hex) to afford the title compound. MS (ESI) 523 (M+H).

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