577778-58-6
Topiroxostat
CAS: 577778-58-6
Molecular Formula: C13H8N6
577778-58-6 - Names and Identifiers
577778-58-6 - Physico-chemical Properties
| Molecular Formula | C13H8N6 |
| Molar Mass | 248.2428 |
| Density | 1.45±0.1 g/cm3(Predicted) |
| Boling Point | 594.7±60.0 °C(Predicted) |
| Solubility | DMSO: 23.5 mg/mL |
| Storage Condition | -20℃ |
| Use | Topilast has a competitive blocking effect on xanthine oxidoreductase, thereby inhibiting uric acid production. It has no blocking effect on other pyrimidine purine metabolizing enzymes, and shows selective blocking effect on xanthine oxidoreductase. Topilast has a significant inhibitory effect on both oxidized and reduced XOR, so its effect of reducing uric acid is more powerful and lasting. Therefore, this product can be used to treat chronic Hyperuricemia of gout. |
577778-58-6 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 4.028 ml | 20.142 ml | 40.283 ml |
| 5 mM | 0.806 ml | 4.028 ml | 8.057 ml |
| 10 mM | 0.403 ml | 2.014 ml | 4.028 ml |
| 5 mM | 0.081 ml | 0.403 ml | 0.806 ml |
Last Update：2024-01-02 23:10:35
577778-58-6 - Preparation
with N2-Boc-Isonicotinic acid hydrazine -1 oxygen (compound 1) and 4-cyanopyridine (compound 2) as starting materials, compound 1 after cyano, compound 4 is obtained by salt formation; Compound 4 and compound 2 are subjected to ring-closing reaction to obtain compound 5 by salt formation. After salt formation and refining, activated carbon is used to remove impurities, alkali is adjusted and dried to obtain a high-purity finished product.
(1) at room temperature, compound 1 and dimethyl carbamoyl chloride were added to acetonitrile, trimethylcyanosilane was added under the protection of nitrogen; The reaction was heated to 60 ℃ for 3H; After the reaction was complete, after the reaction solution is lowered to room temperature, it is poured into water and stirred for crystallization, and the pH value is adjusted to 6-8; After crystallization is completed, it is filtered, the filter cake is washed with water, and the solid is dried to obtain off-white powder, for compound 3.
(2) compound 3 and p-toluenesulfonic acid were added to ethyl acetate for 24h;TLC detection, after the reaction, the solution was white suspension, the solid was filtered, the filter cake was washed with ethyl acetate, drying gave a white solid as compound 4.
(3) compound 2 was dissolved in ethanol, then sodium methoxide was added and reacted at room temperature for 2H; Then compound 4 was added and heated to reflux temperature for 20H; Then, the solution was poured into water, stirred and crystallized, filtered, the filter cake was washed with water, and the light yellow wet product was dried; The wet product was added with P-toluenesulfonic acid methanol: Water: ethyl acetate (5:1:1) mixed solvent, room temperature stirring, the final reaction solution is White suspension, filtered to light yellow solid; Vacuum 80 deg C; Light yellow solid is added methanol: water (6:1) the mixed solvent, nitrogen protection, heating Reflux reaction, after the solid is dissolved clear, add activated carbon Reflux reaction, hot filtration, cooling to room temperature crystallization, drying to a white solid, for compound 5.
(4) compound 5 and sodium carbonate were added to a mixed solvent of acetone/water (volume ratio of 1:1), stirred at room temperature, filtered, and the obtained solid was washed with water, it was dried to give an off-white solid, which was a topirastat drug substance. 2. Isonicotinic acid methyl ester nitrogen oxide was synthesized with Isonicotinic acid nitrogen oxide as raw material and 2-ethoxy-1-ethoxycarbonyl-1, 2-dihydroquinoline as oxidant. Synthesis of 2-cyanoisonicotinic acid methyl ester. 2-cyanoisonicotinic acid methyl ester was hydrolyzed with hydrazine to obtain 2-cyanoisonicotinohydrazide; after the reaction of 4-cyanopyridine with sodium methoxide, the ring-closing reaction of triazole was carried out by docking with 2-cyanoisonicotinohydrazide to obtain the final product of topiramate.
3. The Boc-protected Isonicotinic Acid Hydrazide nitrogen oxide was prepared by condensation reaction of Isonicotinic acid nitrogen oxide with mono-Boc-protected hydrazine, and then reacted with TMSCN to obtain a cyano group, the ring-closing reaction of the triazole was carried out by docking with 4-cyanopyridine to obtain the final product of tropistat.
Last Update：2024-04-09 19:04:54
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