反应详情

A mixture of (S)-2′-oxo-1′,2′,6,8-tetrahydrospiro[cyclopenta[g]quinoline-7,3′-pyrrolo[2,3-b]pyridine]-2-carboxylic acid (15 mg, 0.045 mmol, described in Intermediate 14), 1,2,2a,5-tetrahydropyrrolo[4,3,2-de]quinolin-4(3H)-one, enantiomer B (8 mg, 0.045 mmol, described in Intermediate 19), EDC (13 mg, 0.068 mmol), HOBT (9 mg, 0.068 mmol), and N,N-diisopropylethylamine (0.039 mL, 0.226 mmol) was stirred in DMF (0.7 mL) at ambient temperature for 18 h. The reaction mixture was purified directly by HPLC using a reversed phase C18 column and eluting with a gradient of H2O:CH3CN:CF3CO2H—90:10:0.1 to 5:95:0.1. The pure, product-containing fractions were combined and concentrated to give the title compound. MS: m/z=488 (M+1). HRMS: m/z=488.1703; calculated m/z=488.1717 for C29H22N5O3.

1. customThe reaction mixture was purified directly by HPLC
2. washeluting with a gradient of H2O
3. additionThe pure, product-containing fractions
4. concentrationconcentrated