52486-70-1

Upstream product

• 61295-92-9 methyl 2-cyano-2-hydroxyiminoacetate 

Downstream Products

• 38716-32-4 5-amino-2-(tri-O-benzoyl-β-D-ribofuranosyl)-1(3)H-imidazole-4-carboxylic acid methyl ester 
• 1004-75-7 2,5,6-triamino-4-hydroxypyrimidine 

Relevant academic research and scientific papers

Synthesis process, intermediate and pharmaceutical process of 2, 4, 5-triamino-6-hydroxypyrimidine

The invention discloses a synthesis process of 2, 4, 5-triamino-6-hydroxypyrimidine, which comprises the following steps: 1) carrying out pressurized catalytic hydrogenation reaction on liquid 2-nitroso and 2-methyl cyanoacetate/ethyl cyanoacetate to generate 2-amino and 2-cyanoacetic acid methyl ester/ethyl ester; (2) carrying out cyclization reaction on the 2-amino, 2-methyl cyanoacetate/ethyl cyanoacetate and free guanidine to generate 2, 4, 5-triamino-6-hydroxypyrimidine; wherein the liquid 2-nitroso and 2-methyl cyanoacetate/ethyl cyanoacetate in the step 1) are generated by carrying out nitrosation reaction on methyl cyanoacetate/ethyl cyanoacetate and sodium nitrite. The invention also discloses intermediates 2-nitroso and 2-methyl cyanoacetate in the synthesis process, a synthesis process of the intermediates, and a pharmaceutical process taking the 2, 4, 5-triamino-6-hydroxypyrimidine as an intermediate. According to the present invention, the liquid new compounds such as 2-nitroso and 2-methyl cyanoacetate/ethyl cyanoacetate are subjected to the catalytic hydrogenation reaction, such that the problems of large water consumption and large wastewater yield in the 2, 4, 5-triamino-6-hydroxypyrimidine synthesis process can be solved, and the great economic significance and the great environmental protection significance are provided.

2-amino, 2-methyl cyanoacetate/ethyl cyanoacetate, 2-amino, 2-cyanoacetic acid and synthesis process thereof

The invention discloses a synthesis process of 2-amino, 2-methyl cyanoacetate/ethyl cyanoacetate. The synthesis process comprises the following step: carrying out pressurized catalytic hydrogenation reaction on liquid 2-nitroso and 2-methyl cyanoacetate/ethyl cyanoacetate to generate the 2-amino, 2-methyl cyanoacetate/ethyl cyanoacetate. Wherein the liquid 2-nitroso and 2-methyl cyanoacetate/ethyl cyanoacetate are generated by carrying out nitrosation reaction on methyl cyanoacetate/ethyl cyanoacetate and sodium nitrite. The 2-amino, 2-methyl cyanoacetate/ethyl cyanoacetate can be used as an intermediate in the synthesis process of 2, 4, 5-triamino-6-hydroxypyrimidine, and can be directly subjected to ring closing with guanidyl to generate 2, 4, 5-triamino-6-hydroxypyrimidine, so that the problems of high water consumption and high wastewater yield in the synthesis process can be solved, and great economic significance and environmental protection significance are achieved. In addition, the invention further develops the application of the intermediate, and the intermediate can be used for synthesizing 2, 4, 5-triamino-6-hydroxypyrimidine and guanidyl to generate 2, 4, 5-triamino-6-hydroxypyrimidine, and can also be used for synthesizing 2-amino and 2-cyanoacetic acid.

Enchainements heteroatomiques et leurs produits de cyclisation. VI. Nouvelle synthese de cephemes: acetyl-3 methyl-7 phtalimido-7 oxo-8 thia-5 aza-1 bycyclooctenes-2 diastereomers

The total synthesis of two diastereomeric cephems is described with three original steps in excellent yields: construction of the 1,3-thiazine ring via a (4+2) cycloaddition reaction, regioselective hydrogenation of the carbon-nitrogen double bond, and la