Reaktion #43732

Reaktionsgleichung

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

Lösungsmittel

DMF

Reaktionsbedingungen

Aufarbeitung

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

Vorschrift

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.

Quelle