反応 #43746

反応方程式

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

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.DISSOLUTIONThe product is dissolved in 4M HCl in dioxane
3. 3
   その他dried under high vacuum

実験手順

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.

出典