Water → (S)-1-((S)-2-((S)-2-acrylamidopropanamido)-3,3-dimethylbutanoyl)-N-(4-(3-chloro-2,4-difluorophenylamino)-7-methoxyquinazolin-6-yl)pyrrolidine-2-carboxamide hydrochloride

Participants

Reaction Conditions

Reaction Steps

The compound (30 mg, 0.046 mmol) obtained in Example 12 and NaHCO3 (11.6 mg, 0.14 mmol) were dissolved in THF (0.8 mL): H2O (0.2 mL), and acryloyl chloride (0.004 mL, 0.046 mmol) was added thereto at 0° C. The mixture was stirred at 0° C. for 30 min, and an aqueous solution of NaHCO3 was added thereto, followed by washing several times with chloroform. The organic layer was dried over sodium sulfate, filtered and distilled under reduced pressure, and purified by column chromatography to obtain the title compound (15 mg, 8%).

Provenance & Evidence