6-Fluoro-7-(2-fluoro-4-iodo-phenylamino)-5-oxo-1,2,3,5-tetrahydro-indolizine-8-carboxylic acid (2-tert-butoxy-ethoxy)-amide → 6-Fluoro-7-(2-fluoro-4-iodophenylamino)-N-(2-hydroxyethoxy)-5-oxo-1,2,3,5-tetrahydroindolizine-8-carboxamide

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Reaction Steps

Compound 4a (730 mg, 1.33 mmol) was dissolved in TFA (4 mL) and stirred at r.t. for 1 hour. Purification by prep-HPLC gave 393 mg (60%) of the title compound as a white solid. 1H NMR (400 MHz, DMSO-d6) δ 11.47 (br s, 1H) 8.06 (br s, 1H) 7.58 (dd, 1H, J=10.7, 1.6 Hz) 7.42 (d, 1H, J=8.8 Hz) 6.80 (td, 1H, J=8.7, 2.8 Hz) 4.01 (t, 2H, J=7.3 Hz) 3.77 (t, 2H, J=4.8 Hz) 3.45 (t, 2H, J=4.8 Hz), 3.18 (t, 2H, J=7.7 Hz) 2.11-2.16 (m, 2H). MS (ES) [m+H] calc'd for C17H16F2IN3O4, 492. found 492.

Provenance & Evidence