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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 1962098Generated: October 29, 2026

Water → Nilotinib

https://huagongshe.com/reaction/1962098

Reaction equation

Participants

RoleNameHCIDCharge
ReactantWaterHCID 962—
ReactantNilotinib Hydrochloride AnhydrousHCID 16006490—
SolventMethanolHCID 887—
ProductNilotinibHCID 644241—

Reaction Conditions

Temperature65 °C

Reaction Steps

12 g 4-methyl-N-[3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl]-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-benzamide hydrochloride is dissolved in 192 mL of methanol and 21 ml of water at 52° C. The solution is heated to 64-66° C. in 10 minutes and let stand for 45 minutes. The solution is then cooled down in 3 hours at 0° C. The solution spontaneously crystallized before 0° C.; therefore, the cooling ramp was stopped at 20° C. and let stand with stirring for 2 days. The suspension is cooled down to 0° C. in 2 hours before filtration under vacuum to obtain form A of the hydrochloride salt of 4-methyl-N-[3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl]-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-benzamide.

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS08415363B2
Source datasetuspto-grants-2013_04
ORD IDord-a18f7c6474ae433bab41b8ab1af4b220
Source noteuspto-grants-2013_04