Morpholine → 2-((R)-2-methylmorpholino)-6-(morpholine-4-carbonyl)-8-(1-phenylpyrrolidin-2-yl)-4H-chromen-4-one

TBTU (148 mg, 0.46 mmol) was added to a stirred solution of 2-((R)-2-methylmorpholino)-4-oxo-8-(1-phenylpyrrolidin-2-yl)-4H-chromene-6-carboxylic acid (80 mg, 0.18 mmol), DIPEA (0.080 mL, 0.46 mmol) dissolved in DMA (2 mL) under nitrogen. The resulting solution was stirred at room temperature for 30 min. Morpholine (0.048 mL, 0.55 mmol) was added to the mixture and stirred at room temperature for 1 h. The reaction mixture was purified by preparative HPLC. The fractions containing the desired compound were evaporated to dryness to afford 2-((R)-2-methylmorpholino)-6-(morpholine-4-carbonyl)-8-(1-phenylpyrrolidin-2-yl)-4H-chromen-4-one (60 mg, 65%) as a gummy solid.

1. stirringstirred at room temperature for 1 h
2. customThe reaction mixture was purified by preparative HPLC
3. additionThe fractions containing the desired compound
4. customwere evaporated to dryness

ORDレコード

ord-1d1d702488c84784ab1124a879cffa71

出典データセット

uspto-grants-2013_09

DOI

10.6084/m9.figshare.5104873.v1

特許番号

US08530470B2