Hydrochloric Acid → 2-(4-{[7-(3-chloropropoxy)quinazolin-4-yl]amino}-1H-pyrazol-1-yl)-N-(2-fluorophenyl)acetamide

関与物質

反応手順

Pentafluorophenyl trifluoroacetate (0.325 g, 1.16 mmol) was added dropwise, at room temperature, to a stirred suspension of (4-{[7-(3-chloropropoxy)quinazolin-4-yl]amino}-1H-pyrazol-1-yl)acetic acid (0.300 g, 0.83 mmol) and pyridine (0.092 g, 1.16 mmol) in dimethylformamide (3 ml). After stirring for 5 minutes 2-fluoroaniline (0.184 g, 1.66 mmol) was added and the reaction stirred for 5 hours. The mixture was poured into 0.2N aqueous hydrochloric acid (25 ml) to give 2-(4-{[7-(3-chloropropoxy)quinazolin-4-yl]amino}-1H-pyrazol-1-yl)-N-(2-fluorophenyl)acetamide as a cream coloured solid: MS (+ve ESI): 455 (M+H)+.

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