Tributylphosphine → Ethyl [2-(7-methoxy-5-{[6-(methylsulfonyl)pyridin-3-yl]oxy}-1H-indol-2-yl)-4,5-dihydro-1,3-thiazol-5-yl]acetate

Participants

Reaction Conditions

Reaction Steps

A mixture of 7-methoxy-5-{[6-(methylsulfonyl)pyridin-3-yl]oxy}-1H-indole-2-carbothioamide (10.7 g), ethyl 2-butynoate (8.2 mL), tributylphosphine (7.0 mL) and tetrahydrofuran (400 mL) was stirred at 60° C. for 1 h. The mixture was concentrated under reduced pressure. The residue was purified by silica gel column chromatography (ethyl acetate/hexane=5/95 to 100/0, volume ratio) to give the title compound (11.06 g, 80%) as an orange amorphous solid. MS 490 (MH+).

Provenance & Evidence