1-Hydroxybenzotriazole → HCID 49842494, compound

Participants

Reaction Conditions

Reaction Steps

0.20 g (0.42 mmol) 2-((3R)-4-(tert-butoxycarbonyl)-3-(cycloheptylmethyl)-6-(3,5-difluorophenyl)-2-oxopiperazin-1-yl)ethanoic acid (isomer 4.1.1.1), 0.11 g (0.45 mmol) (R)-5-amino-1,3-dihydrospiro[inden-2,3′-pyrrolo[2,3-b]pyridin]-2′(1′H)-one, 0.11 g (0.55 mmol) 1-ethyl-3-(3-dimethylaminopropyl)-carbodiimide hydrochloride, 74 mg (0.55 mmol) HOBT, 0.06 ml (0.45 mmol) TEA and 2.0 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 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.

Provenance & Evidence