反应详情

400 μL (3.53 mmol) 2,3-dihydro-1H-indole were added to 500 mg (3.17 mmol) 2-chloroisonicotinic acid, 600 μL (3.49 mmol) DIPEA and 1.10 g (3.43 mmol) TBTU in 20 mL THF. The reaction mixture was stirred overnight, diluted with ethyl acetate and washed with 15% potassium carbonate solution (1×), water (1×) and 1M hydrochloric acid (1×). The organic phase was dried on magnesium sulphate, filtered and evaporated down i. vac. The residue was triturated with diisopropylether and suction filtered. The solid was dried at 40° C. in the circulating air dryer.

1. washwashed with 15% potassium carbonate solution (1×), water (1×) and 1M hydrochloric acid (1×)
2. customThe organic phase was dried on magnesium sulphate
3. filtrationfiltered
4. customevaporated down i
5. customThe residue was triturated with diisopropylether and suction
6. filtrationfiltered
7. customThe solid was dried at 40° C. in the circulating air dryer