Compounds having effect of activating SIRT6 deacetylation activity, SIRT6 activator and application of SIRT6 activator
A compound and acetylation technology, applied in organic active ingredients, medical preparations containing active ingredients, organic chemistry, etc., can solve problems such as acetylation activity needs to be improved
- Summary
- Abstract
- Description
- Claims
- Application Information
AI Technical Summary
Problems solved by technology
Method used
Image
Examples
Embodiment 1
[0033] Embodiment 1: the synthesis of compound 1~18
[0034] In this example, the above-mentioned compounds having the structures represented by the formulas (compounds 1-18) are provided. The reaction scheme is as follows:
[0035]
[0036] The specific preparation method is as follows.
[0037] Synthetic Intermediate I: Methyl 2-(N-(5-bromo-4-fluoro-2-methylphenyl)sulfamoyl)-5-nitrobenzoate
[0038]
[0039] At room temperature, the raw material aniline compound (10 g, 49.0 mmol) was dissolved in 20 mL of pyridine, and the raw material 4-nitro-2-carboxymethylbenzenesulfonyl chloride (16.45 g, 58.8 mmol) was added, and the reaction was carried out at room temperature for more than 8 hours. After the completion of the reaction as monitored by TLC, the reaction was cooled to room temperature, and 1N hydrochloric acid was added to adjust the pH to 3-4. A pale yellow precipitate precipitated, which was filtered and dried to obtain the intermediate Int I (18.6 g, yield: 84...
example 1
[0050] Example 1 (compound 1): 2-(N-(5-bromo-4-fluoro-2-methylphenyl)sulfamoyl)-5-((3,5-dichlorophenyl)sulfonyl) benzamide
[0051] 1 H NMR (400MHz, DMSO-d 6 )δ11.28(s,1H),8.78(s,1H),8.35(s,1H),7.97(t,J=1.9Hz,1H),7.94(s,1H),7.77(d,J=2.0 Hz, 2H), 7.39(d, J=8.6Hz, 1H), 7.28–7.12(m, 4H), 1.89(s, 3H). 13 C NMR (101MHz, DMSO) δ170.69, 156.65 (d, J=244.3Hz), 137.24, 136.67, 136.60, 135.59, 134.35 (d, J=4.1Hz), 133.12, 133.04, 133.02, 130.80, 125.60, 110.281, ,118.55(d,J=22.9Hz),104.65(d,J=22.1Hz),17.46.MS(ESI)m / z:609.9(M+H) + .
example 2
[0052] Example 2 (Compound 2): 2-(N-(5-bromo-4-fluoro-2-methylphenyl)sulfamoyl)-5-((3,5-dichlorophenyl)sulfonyl) -N-Methylbenzamide
[0053] 1 H NMR (400MHz, DMSO-d 6 )δ11.30(s,1H),8.85(d,J=6.3Hz,1H),8.80(s,1H),8.01(dt,J=6.4,1.9Hz,1H),7.85(d,J=1.9 Hz,2H),7.47(dd,J=8.9,1.7Hz,1H),7.35(dd,J=8.6,2.4Hz,1H),7.28(t,J=2.4Hz,1H),7.21(d,J =6.7Hz,1H),7.12(dd,J=9.6,3.1Hz,1H),2.68(s,3H),1.90(s,3H). 13 C NMR (101MHz, DMSO) δ167.90, 156.75 (d, J = 244.6Hz), 142.22, 141.74, 137.41, 136.91 (d, J = 7.9Hz), 135.81, 133.72, 132.83 (d, J = 3.1Hz), 131.92 ,131.21,130.90,125.73,119.65,118.73,118.50(d,J=23.0Hz),104.62(d,J=22.1Hz),34.68,17.57.MS(ESI)m / z:623.9(M+H) + .
PUM
Login to View More Abstract
Description
Claims
Application Information
Login to View More