| Molecular Formula | C22H44N6O10 |
| Molar Mass | 552.62 |
| Density | 1.47±0.1 g/cm3(Predicted) |
| Boling Point | 904.0±65.0 °C(Predicted) |
| pKa | 13.07±0.70(Predicted) |
| Physical and Chemical Properties | Chemical properties abbekacin dicarbonate (Ajbekacin Dicarbonate):Q2H44N6O10?2H2CO3. Colorless crystalline powder, melting point 178 ℃ (decomposition). [α]{D24 86.8 °(C = 0.77, water). Acute toxicity LD50 mice (mg/kg):>150 intravenous injection. |
| Use | Use of kanamycin, gentamicin, amikacin resistant bacteria have strong antibacterial activity. For sensitive bacteria caused by sepsis, Pneumonia, etc. |
3,4 '-dideoxykanamycin B and equivalent tert-butoxycarbonyl azide, in a mixed solution of water, pyridine and triethylamine (10:10:1), at room temperature React for 18h. Then, 6 '-N-tert-butoxycarbonyl -3',4 '-dideoxykanamycin B was obtained by Amberlite CG50(NH4 +) column chromatography with 49% yield, melting point 136~140 ℃ (decomposition),[α] {d} 26+112 (C = 1.0, water). At the same time, the 36% unreacted 3 ',4'-dideoxykanamycin B was recovered.
6 '-N-tert-butoxycarbonyl -3',4 '-dideoxykanamycin B(1.1g,2.0 mmo1) and tert-butoxycarbonyl azide (320mg,2.2 mmo1) reacted under the same conditions as above to give 1.41g yellow powder. Without purification, dissolve in 20ml of water and 10ml of dimethoxyethane, acylate with (S)-4-tert-butoxyamino-2-hydroxybutyric acid (N-hydroxysuccinimide) ester (696mg,2.2 mmo1) in a solution of 10ml of dimethoxyethane at room temperature for 20h. React with 10ml 90% trifluoroacetic acid at room temperature for 40min to remove tert-butoxycarbonyl. The reaction solution is concentrated and the product is eluted with Amberlite CG50(NH4 +) column chromatography, eluted with water and 0.5mol/L ammonia water, and then eluted with 0.75mol/L ammonia water. 162mg abbekacin dicarbonate was obtained with 12% yield, melting point 178 ℃ (decomposition),[α]{d} 24+87 (c = 0.77, water).