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56391-57-2生产厂家

56391-57-2价格

56391-57-2

56391-57-2结构式
56391-57-2结构式

化源商城直购

中文名 硫酸奈替米星
英文名 Netilmicin Sulfate
中文别名 1-N-乙基西索米星
硫酸萘替米星USPEP
硫脲嘧啶
英文别名 certomycin
EINECS 260-147-3
(1S,2S,3R,4S,6R)-4-Amino-3-{[(2S,3R)-3-amino-6-(aminomethyl)-3,4-dihydro-2H-pyran-2-yl]oxy}-6-(ethylamino)-2-hydroxycyclohexyl 3-deoxy-4-C-methyl-3-(methylamino)-β-L-arabinopyranoside sulfate (2:5)
1-N-Ethylsisomicin sulfate salt
β-L-Arabinopyranoside, (1S,2S,3R,4S,6R)-4-amino-3-[[(2S,3R)-3-amino-6-(aminomethyl)-3,4-dihydro-2H-pyran-2-yl]oxy]-6-(ethylamino)-2-hydroxycyclohexyl 3-deoxy-4-C-methyl-3-(methylamino)-, sulfate (2 :5) (salt)
Netilmicin sulfate
Zetamicin
MFCD01311715
Netillin
Netilmicin sulfate salt
UNII-S741ZJS97U
Nettacin
Netilmicin (sulfate)
密度 1.32 g/cm3
沸点 684.3ºC at 760 mmHg
熔点 >194ºC (dec.)
分子式 C21H41N5O7.5/2H2O4S
分子量 720.78
闪点 367.7ºC
PSA 814.36000
LogP 1.50400
外观性状 白色至灰白色粉末
储存条件

密封、在2 ºC -8 ºC下保存

稳定性

如果遵照规格使用和储存则不会分解,未有已知危险反应

水溶解性 H2O: soluble10mg/mL | Soluble in water
计算化学

1、 疏水参数计算参考值(XlogP):

2、 氢键供体数量:26

3、 氢键受体数量:44

4、 可旋转化学键数量:16

5、 互变异构体数量:

6、 拓扑分子极性表面积(TPSA):773

7、 重原子数量:91

8、 表面电荷:0

9、 复杂度:754

10、同位素原子数量:0

11、确定原子立构中心数量:22

12、不确定原子立构中心数量:0

13、确定化学键立构中心数量:0

14、不确定化学键立构中心数量:0

15、共价键单元数量:7

更多

1. 性状:白色至淡黄色粉末

2. 密度(g/mL,15ºC):未确定

3. 相对蒸汽密度(g/mL,空气=1):未确定

4. 熔点(ºC):未确定

5. 沸点(ºC):未确定

6. 沸点(ºC,14mmHg):未确定

7. 折射率:未确定

8. 闪点(°C):未确定

9. 比旋光度(ºC):未确定

10. 自燃点或引燃温度(ºC): 未确定

11. 蒸气压(kPa,25ºC):未确定

12. 饱和蒸气压(kPa,60ºC):未确定

13. 燃烧热(KJ/mol):未确定

14. 临界温度(ºC):未确定

15. 临界压力(KPa):未确定

16. 油水(辛醇/水)分配系数的对数值:未确定

17. 爆炸上限(%,V/V):未确定

18. 爆炸下限(%,V/V):未确定

19. 溶解性:极易溶于水,几乎不溶于乙醇及乙醚。

毒理学数据:

LD50(mg/kg)小鼠:静脉注射40,腹腔注射125,皮下注射175[1.19]

生态学数据:

对水是稍微有危害的不要让未稀释或大量的产品接触地下水、水道或者污水系统,若无政府许可,勿将材料排入周围环境。

CHEMICAL IDENTIFICATION

RTECS NUMBER :
WK2286000
CAS REGISTRY NUMBER :
56391-57-2
LAST UPDATED :
199604
DATA ITEMS CITED :
17
MOLECULAR FORMULA :
C21-H41-N5-O7.5/2H2-O4-S
MOLECULAR WEIGHT :
720.80
WISWESSER LINE NOTATION :
T6O BUTJ B1Z EZ FO- BL6TJ AZ CQ EM2 DO- BT6OTJ CQ DM1 EQ E1 ..H2.S-O4

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
>10 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
YKYUA6 Yakkyoku. Pharmacy. (Nanzando, 4-1-11, Yushima, Bunkyo-ku, Tokyo, Japan) V.1- 1950- Volume(issue)/page/year: 36,1249,1985
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
231 mg/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity) Behavioral - ataxia Lungs, Thorax, or Respiration - respiratory stimulation
REFERENCE :
JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 35,461,1982
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
169 mg/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity) Behavioral - ataxia Lungs, Thorax, or Respiration - respiratory stimulation
REFERENCE :
JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 35,461,1982
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
40700 ug/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - effect, not otherwise specified Behavioral - altered sleep time (including change in righting reflex) Lungs, Thorax, or Respiration - respiratory stimulation
REFERENCE :
JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 35,461,1982
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intramuscular
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
167 mg/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity) Behavioral - ataxia Lungs, Thorax, or Respiration - respiratory stimulation
REFERENCE :
JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 35,461,1982
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
189 mg/kg
TOXIC EFFECTS :
Peripheral Nerve and Sensation - flaccid paralysis without anesthesia (usually neuromuscular blockage)
REFERENCE :
AMACCQ Antimicrobial Agents and Chemotherapy. (American Soc. for Microbiology, 1913 I St., NW, Washington, DC 20006) V.1- 1972- Volume(issue)/page/year: 10,827,1976
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
68900 ug/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity) Behavioral - ataxia Lungs, Thorax, or Respiration - respiratory stimulation
REFERENCE :
JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 35,461,1982
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
22 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - effect, not otherwise specified Behavioral - altered sleep time (including change in righting reflex) Lungs, Thorax, or Respiration - respiratory stimulation
REFERENCE :
JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 35,461,1982
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intramuscular
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
63100 ug/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity) Behavioral - ataxia Lungs, Thorax, or Respiration - respiratory stimulation
REFERENCE :
JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 35,461,1982 ** OTHER MULTIPLE DOSE TOXICITY DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intramuscular
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
420 mg/kg/14D-I
TOXIC EFFECTS :
Kidney, Ureter, Bladder - other changes
REFERENCE :
JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 35,461,1982
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intramuscular
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
375 mg/kg/30D-I
TOXIC EFFECTS :
Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) Kidney, Ureter, Bladder - other changes in urine composition Kidney, Ureter, Bladder - changes in bladder weight
REFERENCE :
JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 35,461,1982
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intramuscular
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
1365 mg/kg/26W-I
TOXIC EFFECTS :
Kidney, Ureter, Bladder - interstitial nephritis Kidney, Ureter, Bladder - changes in bladder weight Blood - pigmented or nucleated red blood cells
REFERENCE :
JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 35,499,1982 ** REPRODUCTIVE DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intramuscular
DOSE :
138 mg/kg
SEX/DURATION :
female 7-17 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Newborn - behavioral Reproductive - Effects on Newborn - physical
REFERENCE :
JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 35,614,1982
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intramuscular
DOSE :
550 mg/kg
SEX/DURATION :
female 7-17 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - musculoskeletal system
REFERENCE :
JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 35,614,1982
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intramuscular
DOSE :
650 mg/kg
SEX/DURATION :
female 17-22 day(s) after conception lactating female 21 day(s) post-birth
TOXIC EFFECTS :
Reproductive - Effects on Newborn - weaning or lactation index (e.g., # alive at weaning per # alive at day 4)
REFERENCE :
JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 35,643,1982
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intramuscular
DOSE :
455 mg/kg
SEX/DURATION :
female 6-18 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)
REFERENCE :
JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 35,659,1982 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X4347 No. of Facilities: 25 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 2440 (estimated) No. of Female Employees: 1459 (estimated)

符号 GHS07 GHS08
GHS07, GHS08
信号词 Danger
危害声明 H312 + H332-H360
警示性声明 P201-P261-P280-P308 + P313
个人防护装备 Eyeshields;full-face particle respirator type N100 (US);Gloves;respirator cartridge type N100 (US);type P1 (EN143) respirator filter;type P3 (EN 143) respirator cartridges
危害码 (欧洲) T:Toxic;
风险声明 (欧洲) R60;R20/21/22
安全声明 (欧洲) S53-S36/37/39-S45
危险品运输编码 NONH for all modes of transport
WGK德国 3
RTECS号 WK2286000
海关编码 2942000000

参考文献[12~15]推荐如下路线和方法$

(1)3,2’,6’-三(N-乙酰)西索米星(023-2)的制备

在反应瓶中加入二甲基甲酰胺(DMF)/水的混合溶液100ml(DMF/水,体积比6:2)和乙酸铜5.5g(0.03mol),搅拌悬浮,再加入西索米星(023-1)4.5g(0.01mol),搅拌下加三乙胺调至PH8.5~10.5,在搅拌30min后降温至5 ºC 慢慢滴加乙酸酐3.1g(0.03mol)的3.5mlDMF溶液,滴加时控温在0~10 ºC ,在强烈搅拌下,并不断用三乙胺调节反应液的PH保持8.5~10.5,滴毕,室温(25 ºC)搅拌反应30min~1h.用TLC跟踪显示反应达终点后(如果未达到终点应补乙酸酐的DMF溶液适量),将反应液减压下浓缩,浓缩液用水稀释,冷至(0~10 ºC )保持4h.过滤去固体,滤液用阳离子交换树脂处理,氨水洗脱等处理后得023-2 5.2g,收率90%.

(2)5,2’’,4’’-三(三甲基硅)-3,2’,6’-三(N-乙酰)-西索米星(023-3)的制备

在反应瓶中加入023-2 10g(17.45mmol)、1,2-二甲氧基乙烷(DMF)100ml,搅拌溶解,再加入三甲基氯硅烷25ml(21.15g,194mmol),加热至50 ºC ,搅拌反应16h(在保持50~55 ºC 下)减压蒸除DME,得黄色固体023-3 13.5g,收率93.6%左右,含量91%.经硅胶柱色谱纯化可制得分析试样.

(3)5,2’’,4’’-三(三甲基硅)-1-乙基氨基-3,2’,6’-三(N-乙酰)西索米星(023-5)的制备

在反应瓶中加入化合物023-3 8g(9.5mmol)和水80ml,搅拌溶解,用4mol/L盐酸调至PH6.降温至15 ºC ,加入乙醛2.2ml(1.72g,39mmol),搅拌反应30min,生成亚胺化合物023-4溶液.将NaBH4的水溶液5ml[1g(26.47mmol)NaBH4溶于5ml水]匀速滴入上述含023-4的溶液,并用0.5mol/L盐酸严格控制PH6.继续反应30min,加入0.05mol/L硼砂溶液20ml(PH9.5)继续搅拌1h.得023-5的溶液,含量85%,备用.

(4)O-3-脱氧-4-C-甲基-3-(甲氨基)-B-L-阿拉伯吡喃糖苷(1—6)-O-[2,6-二氨基-2,3,4,6-四脱氧-a-D-甘油己糖-4-烯醇型吡喃糖苷基-(1—4)]-2-脱氧-N’-乙基-D-链霉胺硫酸盐(硫酸奈替米星)(023)的合成

在反应瓶中加入上步制备的含化合物023-5的溶液、珠粒状固体NaOH2g(50mmol)和Na2CO3 2.7g(25.5mmol),搅拌溶解,油浴加热升温至110 ºC ,在该温度下搅拌回流36h.降温至10~15 ºC,加入10mol/L H2SO4调反应液PH至6.5~7.0,抽滤,滤液即为奈替米星游离碱的澄清溶液,含量80%.

在上述澄清溶液中加入阳离子交换树脂,搅拌混合充分后,过滤,用7%氨水洗脱,洗脱液浓缩后用甲醇溶解,再上硅胶柱色谱分离纯化,用氯仿/甲醇/水(40:20:7)洗脱分离.将洗脱液减压浓缩至约10ml,加入活性炭0.5g,恒温水浴加热至50 ºC ,脱色30min.抽滤,滤液用10mol/L H2SO4调至PH3.5~5.5,匀速滴至无水乙醇300ml中,3h后抽滤,滤饼干燥,得023 5.93g,收率78.7,含量在97%以上,符合《中国药典》(2005年版)质量标准.该品为非结晶性固体(冷冻干燥).

56391-57-2 preparation

海关编码 2942000000