Hydrochloric Acid → HCID 178502312, compound

Participants

Reaction Steps

To (1R,3S,4S)-tert-butyl-3-(2′-((S)-1-((S)-2-(methoxycarbonylamino)-3-methylbutanoyl)pyrrolidin-2-yl)-4,5-dihydro-1H,1′H-7,7′-binaphtho[1,2-d]imidazol-2-yl)-2-azabicyclo[2.2.1]heptane-2-carboxylate (307 mg, 0.41 mmol) in DCM (5 mL) and MeOH (1 mL) was added HCl (4M in dioxane, 1 mL). The solution stirred for 2 h, and the solvent was removed. The intermediate (133 mg, 0.2 mmol) was dissolved in DMF (2.5 mL). ((S)-2-(methoxycarbonylamino)-2-(tetrahydro-2H-pyran-4-yl)acetic acid (43 mg, 0.2 mmol), HATU (76 mg, 0.2 mmol), and DIPEA (0.18 mL, 1.0 mmol) were added sequentially. The solution stirred o/n and the mixture was purified by HPLC to yield product (100.8 mg). LCMS-ESI+: calc'd for C48H56N8O7: 857.01 (M+); Found: 857.42 (M+H+).

Provenance & Evidence