Preparation method of triazolopyrimidine sulfydryl type compound
The technology of an azolopyrimidine thiol compound, which is applied in the field of preparation of triazolopyrimidine thiol compounds, can solve the problem of foul-smelling methyl mercaptan, and achieve the effect of being beneficial to industrial production and solving the problem of methyl mercaptan odor
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Embodiment 1
[0020] Preparation of 5-ethoxy-7-fluoro-[1,2,4]-triazolo-[1,5-C]-pyrimidine-2(3H)thione
[0021] Add 10.0g (0.048mol, purity 96%) 5-methoxy-7-fluoro-[1,2,4]-triazolo-[4,3-C]-pyrimidine-3(2H)thione Into 40g ethanol. At 0°C-10°C, 5.4 g of sodium ethoxide was added to the above solution. The mixture was stirred at 0°C-10°C for 2h. Then the mixture was acidified with 9.5 g of 36% concentrated hydrochloric acid, 50 g of water was added, and the mixture was stirred at -5°C for 30 min, and then filtered. The filter cake was washed with 20 ml of cold water and 20 ml of cold ethanol and dried to obtain 9.2 g of the target compound, which was an off-white solid.
[0022] NMR(CDCl 3 )δ: 1 H: 1.47 (t, 3H), 4.69 (q, 2H), 7.04 (d, 1H).
Embodiment 2
[0024] Preparation of 5-ethoxy-7-chloro-[1,2,4]-triazolo-[1,5-C]-pyrimidine-2(3H)thione
[0025] Add 10.8g (0.048mol, 96% purity) 5-methoxy-7-chloro-[1,2,4]-triazolo-[4,3-C]-pyrimidine-3(2H)thione Into 40g ethanol. At 0°C-10°C, 5.4 g of sodium ethoxide was added to the above solution. The mixture was stirred at 0°C-10°C for 2h. Then the mixture was acidified with 9.5g of 36% concentrated hydrochloric acid, 50g of water was added, and the mixture was stirred at below -5°C for 30min and filtered. The filter cake was washed with 20ml of cold water and 20ml of cold ethanol and dried to obtain 9.5g of the target compound. The product was an off-white solid.
Embodiment 3
[0027] Preparation of 5-ethoxy-8-fluoro-[1,2,4]-triazolo-[1,5-C]-pyrimidine-2(3H)thione
[0028] Add 10.0g (0.048mol, 96% purity) 5-methoxy-8-fluoro-[1,2,4]-triazolo-[4,3-C]-pyrimidine-3(2H)thione Into 40g ethanol. At 0°C-10°C, 5.4 g of sodium ethoxide was added to the above solution. The mixture was stirred at 0°C-10°C for 2h. Then the mixture was acidified with 9.5g of 36% concentrated hydrochloric acid, 50g of water was added, and the mixture was stirred at -5°C for 30min, then filtered, and the filter cake was washed with 20ml of cold water and 20ml of cold ethanol and dried to obtain 9.2g of the target compound, which was an off-white solid.
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