Reaktion #89472

Reaktionsgleichung

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

2-fluoro-6-iodobenzoic acid

DIPEA

HATU

→

title compound

2-(((2S,3R)-1-(2-Fluoro-6-iodobenzoyl)-3-methylpiperidin-2-yl)methyl)isoindoline-1,3-dione

Lösungsmittel

ethyl acetate

DMF

Reaktionsbedingungen

Aufarbeitung

1. 1
   Waschenwashed with satd
2. 2
   SonstigeThe organic layer was separated
3. 3
   Trocknendried with MgSO4
4. 4
   Einengenconcentrated in vacuo
5. 5
   SonstigeThe crude product was purified by chromatography on silica gel (EtOAc/hex)

Vorschrift

A mixture of 2-(((2S,3R)-3-methylpiperidin-2-yl)methyl)isoindoline-1,3-dione (0.4 g, 1.549 mmol), 2-fluoro-6-iodobenzoic acid (0.374 g, 1.4 mmol), DIPEA (0.49 mL, 2.8 mmol) and HATU (0.53 g, 1.4 mmol) in DMF (10 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) 507 (M+H).

Quelle