1201676-03-0

1201676-02-9

1201676-03-0

General procedure for the synthesis of 4,6-dichloro-2,3-dihydro-1H-pyrrolo[3,4-c]pyridin-1-one from ethyl 3-(bromomethyl)-2,6-dichloroisonicotinate: a mixture of ethyl 3-(bromomethyl)-2,6-dichloroisonicotinate (13.4 g, 42.7 mmol), tetrahydrofuran (100 mL) and ammonium hydroxide solution (300 mL, 28- 30% ammonia) was stirred at room temperature for 18 hours. After completion of the reaction, the solvent was removed by rotary evaporator. A small amount of water was added to the almost dry solid, which was separated by filtration to obtain a salmon-colored solid, washed sequentially with a small amount of water and ether, and then dried under vacuum. The filtrate was cooled and filtered to give additional salmon-colored solid (7.47 g, 36.8 mmol, 86% yield). Mass spectrum (ESI) m/z 203.2 (M + 1). 1H NMR (400 MHz, DMSO-d6) δ ppm 9.29 (broad single peak, 1H), 7.83 (single peak, 1H), 4.45 (single peak, 2H).