1-(2-Hydroxyethyl)piperazine → 2-[4-(2-Hydroxyethyl)-piperazin-1-yl]-thiazole-5-carboxylic acid methyl ester

To a solution of methyl 2-bromothiazole-5-carboxylate 1 (222 mg, 1.00 mmol) in acetonitrile (20 mL) were added N-(2-hydroxyethyl)piperazine 14c (156 mg, 1.20 mmol) and potassium carbonate (152 mg, 1.10 mmol) under a N2 atmosphere. The reaction mixture was heated to reflux at 80° C. for 10 h. The reaction mixture was filtered through Celite and the filtrate was concentrated under reduced pressure. The residue was purified by column chromatography using silica gel to give the compound 15c (185 mg, 68.2%).

1. temperatureThe reaction mixture was heated
2. filtrationThe reaction mixture was filtered through Celite
3. concentrationthe filtrate was concentrated under reduced pressure
4. customThe residue was purified by column chromatography

ORD record

ord-dcd0bd5e93104dd9bf548dcb30c964eb

Source dataset

uspto-grants-2008_03

DOI

10.6084/m9.figshare.5104873.v1

Patent number

US07345043B2