Acetic Acid → 6-Amino-5-((3-(3-methylfuran-2-carboxamido)phenyl)ethynyl)nicotinic acid

温度

50 °C

Methyl 6-amino-5-((3-(3-methylfuran-2-carboxamido)phenyl)ethynyl)nicotinate (0.550 g, 1.47 mmol) was dissolved in THF (15 mL) and then treated with 1.0 M NaOH (7.33 mL, 7.33 mmol). The reaction mixture was heated to 50° C. Once the reaction was done by TLC, the reaction was cooled to room temperature and then acidified with acetic acid. The reaction mixture was taken up in of EtOAc (˜15 mL) then extracted with H2O (2×15 mL). The water layer then was re-washed with EtOAc (˜15 mL) and the combined organic layers were dried over anhydrous Na2SO4(s). The mixture was then filtered and concentrated in vacuo to give the title compound (0.495 g, 1.37 mmol).

1. temperaturethe reaction was cooled to room temperature
2. extractionthen extracted with H2O (2×15 mL)
3. washThe water layer then was re-washed with EtOAc (˜15 mL)
4. dry with materialthe combined organic layers were dried over anhydrous Na2SO4(s)
5. filtrationThe mixture was then filtered
6. concentrationconcentrated in vacuo

ORDレコード

ord-4f4f4197ce324f12a60acff800a84d38

出典データセット

uspto-grants-2012_03

DOI

10.6084/m9.figshare.5104873.v1

特許番号

US08143410B2