Potassium Phosphate, Tribasic → 5-(4-Chlorophenyl)-1-(4-isopropoxyphenyl)-1H-indole-2-carboxylic acid ethyl ester

A mixture of 5-bromo-3-chloro-1-(4-isopropoxyphenyl)-1H-indole-2-carboxylic acid ethyl ester (see Example 35(b) 402 mg, 1.0 mmol), K3PO4 (716 mg, 3.37 mmol), Pd(OAc)2 (22 mg, 0.1 mmol) and biphenyl-2-yldi-tert-butylphosphine (53 mg, 0.18 mmol) in toluene (10 mL) was stirred at ambient temperature for 10 min after which 4-chlorophenyl boronic acid (233 mg, 1.49 mmol) was added. The reaction was heated at reflux for 5 h, cooled to room temperature and filtered. The filter cake was washed with toluene (5 mL), the combined filtrates were concentrated and the residue was purified by chromatography to afford the sub-title compound (150 mg, 35%).

1. additionwas added
2. temperatureThe reaction was heated
3. temperatureat reflux for 5 h
4. filtrationfiltered
5. washThe filter cake was washed with toluene (5 mL)
6. concentrationthe combined filtrates were concentrated
7. customthe residue was purified by chromatography

ORDレコード

ord-bf86c61d7e194cfc9fbf10ecc9d91c7a

出典データセット

uspto-grants-2010_04

DOI

10.6084/m9.figshare.5104873.v1

特許番号

US07705023B2