反应详情

To a solution of 1 g 5-Methanesulfonyl-1H-indole-2-carboxylic acid methyl ester in 10 ml DMF, 158 mg (60% in oil) sodium hydride were added at RT. After stirring for 10 min 985 mg 2-Bromo-N-(5-chloro-pyridin-2-yl)-acetamide were added and the mixture was stirred for 2 h. After the addition of 7 ml water the mixture was filtered through a chem elut® cartridge by elution with ethyl acetate and concentrated under reduced pressure. The residue was taken-up in 10 ml water/THF 1:2 and treated with 2 ml aqueous KOH solution (10%). After stirring for 16 h at RT the reaction mixture was acidified with hydrochloric acid (5M). The precipitate was collected by filtration and dried in vacuo to yield the product as a yellow solid. Yield: 1.1 g.

1. additionwere added
2. filtrationwas filtered through a chem elut® cartridge by elution with ethyl acetate
3. concentrationconcentrated under reduced pressure
4. additiontreated with 2 ml aqueous KOH solution (10%)
5. stirringAfter stirring for 16 h at RT the reaction mixture
6. filtrationThe precipitate was collected by filtration
7. customdried in vacuo