N-(3-Aminopropyl)morpholine → 1-(4-{4-Cyano-3-[(3-morpholin-4-ylpropyl)amino]isothiazol-5-yl}phenyl)-3-(2-fluoro-5-methylphenyl)urea

Participants

Reaction Conditions

Reaction Steps

A mixture of 1-[4-(3-chloro-4-cyanoisothiazol-5-yl)phenyl]-3-(2-fluoro-5-methylphenyl)urea (50 mg, 0.13 mmol) and 0.2 mL 3-morpholinopropylamine was heated at 70° C. for 18 hours. Then an aqueous Na2CO3/brine mixture and EtOAc workup was done, and the resulting material chromatographed eluting with CHCl3/MeOH. The resulting solid was then triturated with a 1:1/CHCl3/hexane mixture which gave the title compound as a pale yellow solid (10 mg, 16%).

Provenance & Evidence