Pyridine → 1-(4-Isopropoxyphenyl)-5-(5-(trifluoromethyl)pyrid-2-yl)indole-2-carboxylic acid ethyl ester

Anhydrous CH2Cl2 (10 mL), followed by Et3N (92 μL, 0.66 mmol), pyridine (54 μL, 0.66 mmol) and 3 Å molecular sieves (1 g) were added to a mixture of 5-(5-(trifluoromethyl)pyrid-2-yl)indole-2-carboxylic acid ethyl ester (110 mg, 1.33 mmol; see step (b)), Cu(OAc)2 (120 mg, 0.66 mmol), and 4-isopropoxyphenylboronic acid (119 mg, 0.66 mmol). The mixture was stirred vigorously at ambient temperature for 18 h after which additional Cu(OAc)2 (59.9 mg, 0.33 mmol), 4-isopropoxyphenylboronic acid (59.4 mg, 0.33 mmol), Et3N (46.4 μL, 0.33 mmol) and pyridine (27 μL, 0.33 mmol) were added. After a further 30 h of stirring, the mixture was filtered through Celite®. The filter cake was washed with EtOAc and the solvents concentrated and purified by chromatography to give the sub-title compound.

1. additionwere added
2. filtrationthe mixture was filtered through Celite®
3. washThe filter cake was washed with EtOAc
4. concentrationthe solvents concentrated
5. custompurified by chromatography

ORDレコード

ord-483deaccf5da4e09af80aa2847ef220f

出典データセット

uspto-grants-2010_04

DOI

10.6084/m9.figshare.5104873.v1

特許番号

US07705023B2