1-Hydroxybenzotriazole → HCID 22877902, compound

Participants

Reaction Steps

(E)-3-(3-Amino-4-methoxyphenyl)-2-(3,4,5-trimethoxyphenyl)-prop-2-enenitrile hydrochloride (1,007 mg, 2.65 mmols), 1,105 mg of Fmoc-L-Ser(OtBu)OH, 1,370 mg of a BOP reagent and 618 mg of HOBt.H2O were dissolved in 50 ml of acetonitrile, and 0.8 ml of triethylamine were added thereto. The mixture was reacted at 60° C. for 42 hours. One-hundred milliliters of water and a small amount of sodium hydrogencarbonate were added thereto, and the resulting mixture was extracted with ethyl acetate. The extract was washed with a saturated aqueous solution of sodium chloride, then dried over anhydrous sodium sulfate, and concentrated under reduced pressure. The product was purified using a silica-gel column (eluent, mixture of ethyl acetate and hexane at a ratio of 2:3), and then concentrated to produce 1,486 mg (2.14 mmols) of the final product in a yield of 81%.

Provenance & Evidence