6-Aminoindole

• Inhibitors of mammalian target of rapamycin (mTOR ) protein
• Inhibitors of the AcrAB-TolC efflux pump
• Inhibitors of Gli1-mediated transcription in the Hedgehog pathway
• Potent DNA-topoisomerase II poisons and anti-MDR agents
• Protein kinase C θ (PKCθ) inhibitors
• Piperidine carboxamide as transient receptor potential cation channel subfamily V member 1 (TRPV1) antagonists
• Potent and selective blockers of the Nav1.8 sodium channel as potential analgesics for the treatment of neuropathic and inflammatory pain
• 5,6-fused heteroaromatic ureas as TRPV1 antagonists
• Allosteric enhancers of the A3 adenosine receptor
• Human liver glycogen phosphorylase (HLGP) inhibitors for the treatment of type 2 diabetes

4769-96-4

5318-27-4

In Example 1, 6-nitroindole was used as a raw material and reacted at 4.0 MPa hydrogen pressure and 80°C for 48 hours to carry out a hydrogenation reduction reaction. Other steps were the same as in Example 1, and 6-aminoindole was finally obtained in 94% yield. The specific operation was as follows: 16.44 mg (0.04 mmol) of silver 4,4'-dimethoxy-2,2'-bipyridine and 11.22 mg (0.1 mmol) of potassium tert-butoxide were dissolved in 1 mL of 1,4-dioxane and added to an autoclave. After stirring well, 165.15 mg (1 mmol) of m-nitroacetophenone was added and the reaction was stirred at 80 °C for 8 hours. At the end of the reaction, the reaction solution was extracted with water and dichloromethane to separate the organic phase. The organic phase was dried over anhydrous Na2SO4, and then subjected to filtration, rotary evaporation and chromatographic separation to obtain a yellow solid 3-acetanilide in 96% yield.