1,2-Dichloroethane → N-[(3R)-1-(2-cyanobenzyl)piperidin-3-yl]-3-pyridin-4-yl-1-trityl-1H-indazole-5-carboxamide

Participants

Reaction Conditions

Reaction Steps

To a microwave vial equipped with a stir bar was added 3-(pyridin-4-yl)-1-trityl-1H-indazole-5-carboxylic acid (50 mg, 0.104 mmol), HOBT (23.85 mg, 0.156 mmol), EDC (29.9 mg, 0.156 mmol), DIPEA (54.4 μl, 0.311 mmol), 2-{[(3R)-3-aminopiperidin-1-yl]methyl}benzonitrile (22.35 mg, 0.104 mmol), and DMF (1038 μl). The vial was sealed and heated to 40° C. The LCMS taken after 23 hours indicates formation of the desired product. The crude reaction mixture was filtered through a column pre-packed with celite. The material was dry loaded onto 2×10 g columns. The desired product eluted and fractions were collected and concentrated in vacuo.

Provenance & Evidence