Molecular Formula | C6H7N3OS |
Molar Mass | 169.2 |
Density | 1.37 |
Melting Point | 183-184 °C |
Boling Point | 379.7±27.0 °C(Predicted) |
Flash Point | 183.4 °C |
pKa | 2.50±0.10(Predicted) |
Storage Condition | under inert gas (nitrogen or Argon) at 2–8 °C |
Application | 4-amino-2-thiopyrimidine-5-formaldehyde is an intermediate of many medicines and pesticides, it is also a versatile intermediate in organic synthesis. 4-amino -2-thiopyrimidine -5-formaldehyde was used in the synthesis of PamapimodR1487 and homologous p38 mitogen-activated protein kinase inhibitors, this intermediate is also frequently used in many drug molecules and in organic synthesis. |
synthesis method | The preparation steps of 4-amino-2-thiopyrimidine-5-formaldehyde are as follows: 0. 15 to 0. 25mol of cyanoacetaldehyde diethanol acetal or cyanoacetaldehyde dimethanol acetal was dissolved in tetrahydrofuran and added at a temperature of 10-20°C. 20 to 0. 30mol of sodium methoxide was stirred at 10-20°C for 1-2 hours; The reaction was kept warm and slowly added dropwise. 20 to 0.50ml of a 30mol solution of methyl formate in Tetrahydrofuran, and the mixture is stirred at 10-20°C for 5-7 hours after the completion of the dropping; After the above reaction, the mixture is cooled to 10-20°C, then slowly add 0. 20 to 0. 25mol sodium methoxide, raise the temperature to 60-70°C, slowly add Dropwise 0. 15 to 0. 25mol 2-methyl -2-mercaptosulfuric acid urea, after dropping at 60~70°C for 4~6 hours; After the reaction, remove the solvent under reduced pressure, then 80~120ml of a mixture of ethanol and water was added to the reaction system, stirred at 10~20°C for 40~80 minutes and then suction filtered to collect a light yellow solid. The mixture of alcohol and water is washed once and then washed once or twice with water, and dried to give pale yellow crystals, namely 4-amino-2-thiopyrimidine-5-carbaldehyde. |