Trimethylsilylacetylene → 3,4-difluoro-2-[2-fluoro-4-(2-trimethylsilylethynyl)anilino]-N-(2-hydroxyethoxy)-5-[(E)-2-hydroxyethoxyiminomethyl]benzamide

Participants

Reaction Conditions

Reaction Steps

3,4-Difluoro-2-(2-fluoro-4-iodo-phenylamino)-N-(2-hydroxy-ethoxy)-5-[(2-hydroxy-ethoxyimino)-methyl]-benzamide (334 mg, 0.620 mmol) prepared in Example 1 was dissolved in anhydrous tetrahydrofuran (10 mL). (PPh3)2PdCl2 (20,867-1, Sigma-Aldrich Inc.) (21 mg, 0.031 mmol), copper iodide (11 mg, 0.0062 mmol), N,N-diisopropylethylamine (130 μL, 0.774 mmol), and trimethylsilylacetylene (1 mL) were then added thereto at room temperature. The mixture was stirred at 50° C. for two hours.

Provenance & Evidence