2-Amino-5,8-dimethoxy-[1,2,4]triazolo[1,5-c]pyrimidine

To a 100 mL three-necked flask was added 1.5 g of ethyl 4- [4- (2, 5-dimethoxypyrimidinyl)] - 3-thiourea, Hydrochloric acid hydroxylamine 0.5g, 10 mL of 1, 4-dioxane was added, Then, triethylamine (1.2 g)A solution of 0.5 g of sodium methoxide in methanol was further added, The reaction is carried out at 20 ° C to 30 ° C for 10 to 12 hours, HPLC tracking, After completion of the reaction, filter, To give 0.9 g of 2-amino-5, 8-dimethoxy [1, 2, 4] triazolo [1, 5-c] pyrimidine as a white solid, Content of 98.5percent, Yield 91.2percent.Example 4 Example 4 Example 5Preparation of 5, 8-dimethoxy[1, 2, 4]triazolo[1, 5-c]pyrimidin-2-amine (5) 5-Chloro-8-methoxy[1, 2, 4]triazolo[1, 5-c]pyrimidin-2-amine (4; 100 mg, 0.50 mmol) was suspended in acetonitrile (5 mL) at room temperature and treated with 25percent sodium methoxide in methanol (200 mg, 2 eq). The resulting slurry was stirred at room temperature for 1.5 hours and then filtered. The solids were washed with water and dried to afford the title compound as a chalk-colored solid (87 mg, 88percent) that was identical in HPLC retention to authentic 5, 8-dimethoxy[1, 2, 4]triazolo[1, 5-c]pyrimidin-2-amine (5): mp 185-186° C.; To a 100 mL three-necked flask was added 1.5 g of ethyl 4- [4- (2, 5-dimethoxypyrimidinyl)] - 3-thiourea, Hydrochloric acid hydroxylamine 0.5g, 10 mL of 1, 4-dioxane was added, Then, triethylamine (1.2 g)A solution of 0.5 g of sodium methoxide in methanol was further added, The reaction is carried out at 20 ° C to 30 ° C for 10 to 12 hours, HPLC tracking, After completion of the reaction, filter, To give 0.9 g of 2-amino-5, 8-dimethoxy [1, 2, 4] triazolo [1, 5-c] pyrimidine as a white solid, Content of 98.5percent, Yield 91.2percent.Example 4 Example 4 Example 5Preparation of 5, 8-dimethoxy[1, 2, 4]triazolo[1, 5-c]pyrimidin-2-amine (5) 5-Chloro-8-methoxy[1, 2, 4]triazolo[1, 5-c]pyrimidin-2-amine (4; 100 mg, 0.50 mmol) was suspended in acetonitrile (5 mL) at room temperature and treated with 25percent sodium methoxide in methanol (200 mg, 2 eq). The resulting slurry was stirred at room temperature for 1.5 hours and then filtered. The solids were washed with water and dried to afford the title compound as a chalk-colored solid (87 mg, 88percent) that was identical in HPLC retention to authentic 5, 8-dimethoxy[1, 2, 4]triazolo[1, 5-c]pyrimidin-2-amine (5): mp 185-186° C.;

Molecular Weight:195.18
Hydrogen Bond Donor Count:1
Hydrogen Bond Acceptor Count:6
Rotatable Bond Count:2
Exact Mass:195.07562455
Monoisotopic Mass:195.07562455
Topological Polar Surface Area:87.6
Heavy Atom Count:14
Complexity:205
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes