1-Hydroxybenzotriazole → HCID 49842493, compound

Participants

Reaction Conditions

Reaction Steps

0.10 g (0.22 mmol) 2-(4-(tert-butoxycarbonyl)-6-(3,5-difluorophenyl)-2-oxo-3-(tetrahydro-2H-pyran-4-yl)piperazin-1-yl)ethanoic acid (isomer mixture 1.1.1), 60 mg (0.24 mmol) (R)-5-amino-1,3-dihydrospiro[indene-2,3′-pyrrolo[2,3-b]pyridin]-2′(1′H)-one, 58 mg (0.30 mmol) 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide-hydrochloride, 41 mg (0.30 mmol) HOBT, 0.03 ml (0.24 mmol) TEA and 1.5 ml DMF were stirred overnight at RT. The reaction mixture was concentrated by rotary evaporation. The residue was stirred with 15 ml of a 1.25M methanolic hydrochloric acid solution for 1 h at 50° C. The mixture was concentrated by rotary evaporation and the residue was purified by HPLC. The product-containing fractions were combined and lyophilised. The product was obtained as an isomer mixture.

Provenance & Evidence