4-Fluorobenzylamine → 2-chloro-6-(4-fluorobenzyl)-5H-pyrrolo[3,4-b]pyridin-7(6H)-one

Participants

Reaction Steps

A solution of methyl 3-(bromomethyl)-6-chloropicolinate (100 mg, 0.38 mmol) and 4-fluorobenzylamine (237 mg, 1.89 mmol) in MeOH (10 mL) was stirred at 15° C. overnight. After the reaction, it was filtered to afford crude 2-chloro-6-(4-fluorobenzyl)-5H-pyrrolo[3,4-b]pyridin-7(6H)-one (75 mg, yield: 72%). 1H-NMR (CDCl3, 400 MHz) δ 7.73 (d, J=8.0 Hz, 1H), 7.47 (d, J=8.0 Hz, 1H), 7.28˜7.31 (m, 2H), 7.05 (t, J=8.4 Hz, 2H), 4.82 (s, 2H), 4.25 (s, 2H). MS (M+H)+: 277/279.

Provenance & Evidence