Application of compound as JAK-STAT3 signal passage inhibitor
A technology of JAK-STAT3 and signaling pathways, which is applied in the direction of drug combinations, medical preparations containing active ingredients, organic active ingredients, etc., can solve the problems that have not yet been clinically treated for cancer, and achieve the effect of improving prognosis and improving curative effect
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Embodiment 1
[0150] 5-Chloro-N-(4-fluorophenyl)-2-hydroxybenzamide
[0151] (5-chloro-N-(4-fluorophenyl)-2-hydroxybenzamide)
[0152]
[0153] resolve resolution:
[0154] Mix 1 mmol of 5-chloro-2-methoxybenzoic acid and 2 ml of thionyl chloride and heat to reflux for one hour. Thionyl chloride was distilled off, then diluted with 2 ml of anhydrous tetrahydrofuran, and then used.
[0155] 2 mmol of 4-fluoroaniline compounds were dissolved in 2 ml of anhydrous tetrahydrofuran, and then added dropwise to the previously prepared 5-chloro-2-methoxybenzoyl chloride solution at room temperature, and stirred overnight at room temperature. After the reaction was detected by thin layer chromatography, at room temperature, an appropriate amount of water and dichloromethane were added, the mixture was transferred to a separatory funnel, and the organic layer was taken. The organic layer solution was washed successively with appropriate amount of dilute sodium hydroxide solution (once), saturate...
Embodiment 2
[0160] 5-Chloro-N-(3,4-difluorophenyl)-2-hydroxybenzamide
[0161] (5-chloro-N-(3,4-difluorophenyl)-2-hydroxybenzamide)
[0162]
[0163] The synthesis method is as in Example 1.
[0164] 1 HNMR (400MHz, DMSO-d 6 ), δ11.60(s, 1H), 10.52(s, 1H), 7.86~7.91(m, 2H), 7.43~7.48(m, 3H), 7.46~7.49(m, 1H), 7.02(d, J = 1.6Hz, 1H)
[0165] MS(ES+APCI), m / z: 284.1(M+H) + , 282.0(M-H) -
Embodiment 3
[0167] 5-Chloro-N-(4-(4-morpholinyl)phenyl)-2-hydroxybenzamide
[0168]
[0169] The synthesis method is as in Example 1.
[0170] 1 HNMR (400MHz, DMSO-d 6 ), δ10.41(s, 1H), 7.99(d, J=2.0Hz, 1H), 7.54(d, J=8.8Hz, 2H), 7.43~7.46(m, 1H), 6.94~6.99(m, 3H),
[0171] MS(ES+APCI), m / z: 333.0(M+H) + , 331.2(M-H) -
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