反応 #43732

反応方程式

5,7-dichlorobenzofuran-2-carboxylic acid

HATU

N,N-diisopropylethylamine

→

title compound

N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]-5,7-dichloro-1-benzofuran-2-carboxamide hydrochloride

溶媒

DMF

反応条件

後処理

1. 1
   その他The reaction mixture is purified by preparative HPLC
2. 2
   workup.ADDITIONAn excess of 1N hydrochloric acid is then added to the product
3. 3
   その他The solvent is removed under reduced pressure

実験手順

227 mg (0.98 mmol) of 5,7-dichlorobenzofuran-2-carboxylic acid, 200 mg (0.98mmol) of R-3-aminoquinuclidine dihydrochloride, 449 mg (1.18 mmol) of HATU, 458 mg (3.54 mmol) of N,N-diisopropylethylamine and 2.0 ml of DMF are reacted according to the general procedure (variant B). The reaction mixture is purified by preparative HPLC. An excess of 1N hydrochloric acid is then added to the product. The solvent is removed under reduced pressure. 169 mg (46% of theory) of the title compound are isolated.

出典