2-Fluoroisoniazide
2-Fluoroisoniazide Basic information
- Product Name:
- 2-Fluoroisoniazide
- Synonyms:
-
- 2-Fluoroisoniazide
- 2-Fluoropyridine-4-carbohydrazide
- 2-fluoroisonicotinohydrazide
- 4-Pyridinecarboxylicacid, 2-fluoro-, hydrazide
- 2-FLUOROISONICOTINIC ACID HYDRAZIDE
- 2-fluoro-4-pyridinecarbohydrazide
- CAS:
- 369-24-4
- MF:
- C6H6FN3O
- MW:
- 155.13
- Mol File:
- 369-24-4.mol
2-Fluoroisoniazide Chemical Properties
- Melting point:
- 218-220 °C
- Density
- 1.356±0.06 g/cm3(Predicted)
- pka
- 10.53±0.10(Predicted)
2-Fluoroisoniazide Usage And Synthesis
Application
2-Fluoroisoniazid and para-aminosalicylic acid isoniazid have become alternative drugs, but the vast majority of doctors still consider 2-fluoroisoniazid an indispensable primary drug for the treatment of tuberculosis. It is considered a first-line anti-tuberculosis drug, along with rifampicin, ethambutol, streptomycin, and pyrazinamide.
Synthesis
To 2000ml three-necked bottle add 1.62mol 2-fluoroisonicotinic acid, 1200g ethanol, 16.4g (0.162mol) triethylamine, stirring to lower the temperature to 0 ?? C ~ 5 ?? C, slowly drop 212g (1.78mol) sulfoxide chloride, dropletting is completed, controlled temperature 0 ?? C ~ 5 ?? C insulation for 2 hours, and then warmed up to 20 ?? C ~ 25 ?? C insulation for 20 hours, the reaction is complete, the Decompression concentration of the oil, will be 119g (2.43mol) hydrazine hydrate to add, warming to 70 ?? ~ 75 ??, holding 10 hours, add diluent (water 350g), appropriate warming, dissolution, to get aqueous solution of 2-fluoroisonicotinic acid hydrazide crude, add 10g of activated charcoal, 70 ?? ~ 75 ?? holding time of half an hour, filtration, filtrate is naturally cooled for 6 hours, and then slowly cooled to 0 ??, filtration The filtrate was naturally cooled for 6 hours, then slowly cooled to 0??C, filtered and dried to obtain the finished product of isoniazid with the purity of 99.94%, the single impurities were all less than 0.10%, the impurity J was not detected, and the total yield of 2-fluoroisonicotinic acid hydrazide was 86%.
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