Reaktion #43754

Reaktionsgleichung

7-chloro-1-benzothiophene-2-carboxylic acid

HATU

N,N-diisopropylethylamine

→

title compound

N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]-7-chloro-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 a mixture of 4M HCl in dioxane and methanol
3. 3
   Einengenconcentrated

Vorschrift

176.2 mg (0.83 mmol) of 7-chloro-1-benzothiophene-2-carboxylic acid, 150 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 a mixture of 4M HCl in dioxane and methanol and then concentrated. 175.2 mg (65.1% of theory) of the title compound are obtained.

Quelle