Novel oxalyl piperazines active against the hepatitis b virus (HBV)
A compound and solvate technology, applied in the field of new antiviral agents, can solve problems such as low solubility, lack of selectivity, and mutagenicity
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[0570] Preparation of 4-cyano-1H-indole-2-carboxylic acid
[0571]
[0572] Step J: To a stirred solution of compound 11 (5.00 g, 19.7 mmol) in DMF (50 mL) was added CuCN (3.00 g, 33.5 mmol). The mixture was stirred at 150 °C for 4 h. The mixture was then cooled to room temperature, and water (100 mL) was added. The resulting mixture was extracted with ethyl acetate (4 x 100 mL). The combined organic extracts were washed with water (50 mL) and brine (50 mL), washed with Na 2 SO 4 Drying and evaporation under reduced pressure yielded 2.50 g (12.5 mmol, 63%) of compound 12, which was pure enough for the next step.
[0573] Step K: To a solution of compound 12 (2.50 g, 12.5 mmol) in ethanol (30 mL) was added LiOH·H 2 O (0.600 g, 13.0 mmol). The mixture was refluxed for 10 h. The solvent was evaporated under reduced pressure and the residue was diluted with water (50 mL). The aqueous layer was acidified to pH 6 with 10% aqueous hydrochloric acid, and the precipitated so...
Embodiment 1
[0954] N-(3-bromophenyl)-2-[4-(1H-indole-2-carbonyl)piperazin-1-yl]-2-oxoacetamide
[0955]
Embodiment 5
[0957] 2-[4-(7-Bromo-1H-indole-2-carbonyl)piperazin-1-yl]-N-butyl-2-oxoacetamide
[0958]
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