153773-82-1
153773-82-1 結(jié)構(gòu)式
基本信息
厄他培南粗品
厄他培南鈉鹽
(4R,5S,6S)-3-[[(3S,5S)-5-[[(3-羧基苯基)氨基甲?；鵠吡咯烷-3-基]硫-6-(1-羥基乙基)-4-甲基-7-氧代-1-氮雜雙環(huán)[3.2.0]庚-2-烯-2-甲酸鈉鹽
(4R,5R,6S)-3-[(3S,5S)-5-[(3-羧基苯基)氨基甲?；鵠吡咯烷-3-基]硫-6-(1-羥乙基)-4-甲基-7-氧代-1-氮雜雙環(huán)[3.2.0]庚-2-烯-2-甲酸鈉鹽/厄他培南鈉鹽/爾他培南鈉鹽/呃他培南鈉鹽
3-(((3S
L 749345
EtapeneM
Etapenem sodium
ErtapeneM Crude
ErtapeneM MonosodiuM
Ertapenem Impurity 16
Ertapenem sodium, >=97%
He Seoul sodium imipenem
物理化學(xué)性質(zhì)
制備方法
202467-70-7
153773-82-1
以化合物（CAS: 202467-70-7）為原料，按照CN102731508A中所述的方法，合成(4R,5S,6S)-3-(((3S,5S)-5-((3-羧基苯基)氨基甲?；?吡咯烷-3-基)硫基)-6-((R)-1-羥乙基)-4-甲基-7-氧代-1-氮雜雙環(huán)[3.2.0]庚烷-2-烯-2-甲酸單鈉鹽的一般步驟如下：在750 mL乙酸乙酯和500 mL水的混合溶劑中，加入實施例1制備的雙重保護的厄他培南晶體形式（10 g，0.017 mol）。用5%氫氧化鈉水溶液調(diào)節(jié)pH至7.1-7.2，隨后加入15 g鈀碳催化劑。在氫氣壓力為20.0-30.0 MPa的條件下氫化反應(yīng)2小時。反應(yīng)完成后，過濾去除催化劑，濾液用二氯甲烷（100 mL×2）萃取，分離水層。水層通過大孔吸附樹脂進行吸附，隨后用2 L去離子水洗滌樹脂。接著，用含0.05 M碳酸氫鈉的丙酮溶液洗脫，洗脫液酸化至pH 5.5后，采用納濾法濃縮至50 mL。向濃縮液中加入100 g甲醇與正丙醇的混合溶劑（W/W = 1:1），進一步濃縮促進結(jié)晶。結(jié)晶過程溫度控制在10-20℃，結(jié)晶完成后過濾收集產(chǎn)物。產(chǎn)物在<0.09 MPa的真空條件下干燥3小時，最終得到厄他培南單鈉鹽3.4 g，收率為40.2%，HPLC純度為99.2%。
參考文獻：
[1] Patent: CN104788452, 2017, B. Location in patent: Paragraph 0067; 0068
[2] Patent: WO2013/121279, 2013, A2. Location in patent: Page/Page column 15
| 報價日期 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS號 | 包裝 | 價格 |
| 2025/05/22 | HY-13625 | 厄他培南鈉 Ertapenem sodium | 153773-82-1 | 1 mg | 187元 |
| 2025/05/22 | HY-13625 | 厄他培南鈉 Ertapenem sodium | 153773-82-1 | 5 mg | 375元 |
| 2025/05/22 | HY-13625 | 厄他培南鈉 Ertapenem sodium | 153773-82-1 | 10 mg | 600元 |
常見問題列表
Ertapenem sodium inhibits
Streptococcus pneumoniae
with MIC
50
s values < 1mg/L.
Ertapenem sodium exhibits a bactericidal mode of action as shown by time-killing curves and exhibits a short postantibiotic effect (PAE) of 1.4-2.6 h against the Gram-positive strains but no PAE against Gram-negative strains.
Ertapenem sodium (50 mg/kg; s.c.; q6h; for 24 hours) shows substantial bactericidal activity against
S. pneumoniae
in the murine thigh infection model.
Ertapenem sodium exhibits an AUC
0-24
of 586 mg?h/L, C
max
of 140 mg/L following subcutaneous injection (mice 50 mg/kg).
| Animal Model: | Specific-pathogen-free female ICR mice (~25 g), thigh infection model |
| Dosage: | 50 mg/kg |
| Administration: | Subcutaneous injection, q6h, for 24 hours |
| Result: | Showed substantial bactericidal activities. |
| Animal Model: | Specific-pathogen-free female ICR mice (~25 g), thigh infection model |
| Dosage: | 20 mg/kg, 50 mg/kg, 100 mg/kg (Pharmacokinetic Analysis) |
| Administration: | Subcutaneous injection |
| Result: | AUC 0-24 (586 mg?h/L), C max (140 mg/L) at 50 mg/kg q6h dosing regimen. |