2-CHLORO-7H-PYRROLO[2,3-D]PYRIMIDINE

90213-66-4

335654-06-3

The general procedure for the synthesis of 2-chloro-7H-pyrrolo[2,3-d]pyrimidines from 2,4-dichloro-7H-pyrrolo[2,3-d]pyrimidines is as follows: zinc powder (8700.0 g, 133 mol, 10.0 eq.) was added in batches to glacial acetic acid (3.3 L, 53.2 mol, 4.0 eq.), followed by addition of acetonitrile (30.0 L) to form a reaction mixture. The reaction mixture was cooled to 25 °C and then filtered. The filtrate was concentrated under reduced pressure and then added to 30 L of ice water to precipitate the product. The mixture was warmed to 80 °C and kept at this temperature for 14 hours. Upon completion of the reaction, a pink solid was obtained. The solid was collected by filtration and the cake was washed with water (5 L x 3 times) and dried to give 1501.7 g of white solid in 73.54% yield.