反応 #43765

反応方程式

triethylamine

benzenesulfonyl chloride

N-[(3R)-1-azabicyclo[2.2.2]oct-3-yl]-6-amino-1-benzo-thiophene-2-carboxamide hydrochloride

→

title compound

N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]-6-[bis(phenylsulfonyl)amino]-1-benzo-thiophene-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 a mixture of 1N aqueous hydrochloric acid and acetonitrile
3. 3
   濃縮again concentrated
4. 4
   その他dried under high vacuum

実験手順

40 mg (0.11 mmol) of N-[(3R)-1-azabicyclo[2.2.2]oct-3-yl]-6-amino-1-benzo-thiophene-2-carboxamide hydrochloride are dissolved in 2 ml of DMF, 6.5 mg (0.05 mmol) of N,N-dimethyl-4-aminopyridine, 59.6 μl (0.43 mmol) of triethylamine and 27.2 μl (0.21 mmol) of benzenesulfonyl chloride are added and the mixture is stirred at room temperature for 16 h. The reaction mixture is purified by preparative HPLC. The product is dissolved in a mixture of 1N aqueous hydrochloric acid and acetonitrile, then again concentrated and dried under high vacuum. 33 mg (50% of theory) of the title compound are obtained.

出典