1-Hydroxybenzotriazole → 2-((R)-3-(3,5-difluorophenyl)-1-methyl-5-oxo-8,11-dioxa-1,4-diazaspiro[5.6]dodecan-4-yl)-N-((R)-2'-oxo-1,1',2',3-tetrahydrospiro[inden-2,3'-pyrrolo[2,3-b]pyridin]-5-yl)acetamide

Participants

Reaction Conditions

Reaction Steps

75 mg (0.20 mmol) (R)-2-(3-(3,5-difluorophenyl)-1-methyl-5-oxo-8,11-dioxa-1,4-diazaspiro[5.6]dodecan-4-yl)-ethanoic acid, 55 mg (0.22 mmol) (R)-5-amino-1,3-dihydrospiro[inden-2,3′-pyrrolo[2,3-b]pyridin]-2′(1′H)-one, 50 mg (0.26 mmol) 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide-hydrochloride, 35 mg (0.26 mmol) HOBT, 0.07 ml (0.50 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 for 1 h at 50° C. The mixture was concentrated by rotary evaporation and the residue was purified by HPLC. The fractions containing the product were combined and lyophilised.

Provenance & Evidence