Isopropylamine → 6-{[2-(3-chloro-pyridin-2-yl)-5-trifluoromethyl-2H-pyrazole-3-carbonyl]-amino}-5-cyano-1H-indazole-7-carboxylic acid isopropylamide

Participants

Reaction Steps

To a mixture of 426 mg of the above 7-[2-(3-chloro-pyridin-2-yl)-5-trifluoromethyl-2H-pyrazol-3-yl]-5-ethynyl-1H-8-oxa-1,2,6-triaza-cyclopenta[a]naphthalen-9-one in 7 mL of 4:1 (v/v) mixture of acetonitrile/water is added 0.79 mL (9.3 mmol) of isopropylamine. The reaction mixture is stirred during 4 hours at ambient temperature and then concentrated in vacuo. After purification by flash chromatography (SiO2, hexane/ethyl acetate 4:1), 250 mg (38%) of product are obtained as a yellow solid; LC/MS:516/518 (M+H)+; m.p.: 226-229° C.

Provenance & Evidence