Reaktion #43746

Reaktionsgleichung

3-chloro-6-fluoro-1-benzothiophene-2-carboxylic acid

HATU

N,N-diisopropylethylamine

→

title compound

N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]-3-chloro-6-fluoro-1-benzothiophene-2-carboxamide hydrochloride

Lösungsmittel

DMF

Reaktionsbedingungen

Aufarbeitung

1. 1
   SonstigeThe reaction mixture is purified by preparative HPLC
2. 2
   workup.DISSOLUTIONThe product is dissolved in 4M HCl in dioxane
3. 3
   Sonstigedried under high vacuum

Vorschrift

191.1 mg (0.83 mmol) of 3-chloro-6-fluoro-1-benzothiophene-2-carboxylic acid, 150.0 mg (0.75 mmol) of R-3-aminoquinuclidine dihydrochloride, 343.7 mg (0.90 mmol) of HATU, 350.5 mg (2.71 mmol) of N,N-diisopropylethylamine and 3.0 ml of DMF are reacted according to the general procedure (variant B). The reaction mixture is purified by preparative HPLC. The product is dissolved in 4M HCl in dioxane, then reconcentrated and dried under high vacuum. 223.3 mg (77.4% of theory) of the title compound are obtained.

Quelle