A kind of compound against Cva16 type hand, foot and mouth disease and synthesis method thereof
A synthesis method and compound technology, applied in antiviral agents, organic chemistry, etc., can solve the problems of insufficient etiological research and less attention than EV71.
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Embodiment 1
[0036] Embodiment 1. Synthetic approach and conditions of the compound shown in formula (I) of the present invention
[0037] The synthetic route is as follows:
[0038]
[0039] step 1.
[0040] Add compound 1 o-hydroxybenzoic acid (1.38g, 10mmol) in the 50ml round bottom flask, succinic anhydride (1.2g, 12mmol), pyridine 15ml, catalyst DMAP (4-dimethylaminopyridine, 1.46g, 12mmol) is, is heated to React at 90°C for 5h.
[0041] After the reaction was completed, the solvent was distilled off under reduced pressure, and dichloromethane:methanol (volume ratio 2:1) was used as the mobile phase column chromatography to obtain compound 2.
[0042] Step 2.
[0043] Add compound 2 (2.38g, 10mmol) in the 50ml round bottom flask, compound 3 (Cas#111-77-3, diethylene glycol monomethyl ether, 1.4g, 12mmol), catalyst DCC (dicyclohexylcarbodiimide , 2.47g, 12mmol) and dichloromethane (5ml). Heated to reflux and reacted for 12h. After the reaction was completed, the solvent was di...
Embodiment 2
[0052] Embodiment 2. Derivatives of compounds shown in formula (I) of the present invention
[0053] Derivatives of Compound I
[0054] Wherein, R is methyl, ethyl, carboxymethyl, nitro, methoxy, formyl, acetyl, formamido, acetamido or phenyl.
[0055] Synthetic route is with embodiment 1.
[0056] step 1.
[0057] Add compound 1 (1.38g, 10mmol), succinic anhydride (1.2g, 12mmol), pyridine 15ml, catalyst DMAP (4-dimethylaminopyridine, 1.46g, 12mmol) into a 50ml round bottom flask, heat to 90°C for 5h .
[0058] After the reaction was completed, the solvent was distilled off under reduced pressure, and dichloromethane:methanol (volume ratio 2:1) was used as the mobile phase column chromatography to obtain compound 2.
[0059] Compound 1 is Wherein R is methyl, ethyl, carboxymethyl, nitro, methoxy, formyl, acetyl, formamido, acetamido or phenyl.
[0060] Step 2.
[0061] Add compound 2 (2.38g, 10mmol) in the 50ml round bottom flask, compound 3 (Cas#111-77-3, diethylene...
experiment example 1
[0065] Experimental example 1 Detection of antiviral activity of the compound of formula (I) of the present invention.
[0066] In order to detect the in vitro antiviral activity of the test compound, CVA 16 was isolated from clinical specimens of hand, foot and mouth, and the test compound was artificially reconfirmed in vitro antiviral activity by plaque test.
[0067] Will 1×10 6 RD cells per well (human malignant embryonic rhabdomyosarcoma cells, Cat NO.: CL-0193, tissue source: muscle, rhabdomyosarcoma) were inoculated in 6-well plates, after overnight culture, the virus solution to be tested was diluted 10 times Infect RD cells, repeat 3 wells for each dilution, remove the supernatant after infection at 37°C for 1 h, add semi-solid medium containing 1.2% methylcellulose, 2% serum (DMEM high glucose (product number: PM150210) + 10% FBS (product number: 164210-500) + 1% P / S (product number: PB180120)), placed in an incubator for 5-6 days until virus plaques are formed.
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