苯磺酸氨氯地平
苯磺酸氨氯地平用途
苯磺酸氨氯地平名称
[ CAS 号 ]:
111470-99-6
[ 中文名 ]:
2[(2-氨基乙氧基)甲基]-4(2-氯苯基)-3-乙氧甲酰基-5-甲氧甲酰基-6-甲基-1,4-二氢吡啶苯磺酸盐
[ 英文名 ]:
Amlodipine besylate
[中文别名 ]:
[英文别名 ]:
- Amlodin
- Norvasc
- UNII:864V2Q084H
- MFCD00887594
- Amlodipine Besilate
- Amlodipine besylate
- AMLODIPINE BENZENESULFONATE
苯磺酸氨氯地平生物活性
[ 描述 ]:
[ 相关类别 ]:
[参考文献]
[相关活性小分子]
苯磺酸氨氯地平物理化学性质
[ 密度 ]:
1.227g/cm3
[ 沸点 ]:
527.2ºC at 760 mmHg
[ 熔点 ]:
199-201°C
[ 分子式 ]:
C26H31ClN2O8S
[ 分子量 ]:
567.051
[ 闪点 ]:
272.6ºC
[ 精确质量 ]:
566.148987
[ PSA ]:
162.63000
[ LogP ]:
5.30950
[ 外观性状 ]:
白色粉末
[ 蒸汽压 ]:
3.34E-11mmHg at 25°C
[ 储存条件 ]:
Store at RT
[ 水溶解性 ]:
DMSO: 20 mg/mL
苯磺酸氨氯地平MSDS
苯磺酸氨氯地平毒性和生态
CHEMICAL IDENTIFICATION
- RTECS NUMBER :
- US7967700
- CHEMICAL NAME :
- 3,5-Pyridinedicarboxylic acid, 2-((2-aminoethoxy)methyl)-4-(2-chlorophenyl)- 1,4-dihydro-6-methyl-, 3-ethyl-5-methyl ester, monobenzenesulfonate
- CAS REGISTRY NUMBER :
- 111470-99-6
- LAST UPDATED :
- 199806
- DATA ITEMS CITED :
- 12
- MOLECULAR FORMULA :
- C20-H25-Cl-N2-O5.C6-H6-O3-S
- MOLECULAR WEIGHT :
- 567.10
HEALTH HAZARD DATA
ACUTE TOXICITY DATA
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Unreported
- SPECIES OBSERVED :
- Human - woman
- DOSE/DURATION :
- 6 mg/kg/60D-I
- TOXIC EFFECTS :
- Sense Organs and Special Senses (Olfaction) - effect, not otherwise specified
- REFERENCE :
- LANCAO Lancet. (7 Adam St., London WC2N 6AD, UK) V.1- 1823- Volume(issue)/page/year: 341,1102,1993
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 393 mg/kg
- TOXIC EFFECTS :
- Sense Organs and Special Senses (Eye) - ptosis Lungs, Thorax, or Respiration - respiratory depression Blood - other changes
- REFERENCE :
- OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 42,177,1991
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intraperitoneal
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 42 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,71,1995
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Subcutaneous
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 678 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,71,1995
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 37 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,71,1995
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intraperitoneal
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 31 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,71,1995
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Subcutaneous
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 36 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,71,1995 ** OTHER MULTIPLE DOSE TOXICITY DATA **
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 910 mg/kg/13W-C
- TOXIC EFFECTS :
- Kidney, Ureter, Bladder - urine volume increased Kidney, Ureter, Bladder - other changes in urine composition
- REFERENCE :
- OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 42,177,1991
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 36400 mg/kg/52W-C
- TOXIC EFFECTS :
- Kidney, Ureter, Bladder - urine volume increased Kidney, Ureter, Bladder - other changes in urine composition Related to Chronic Data - death
- REFERENCE :
- OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 42,177,1991 ** REPRODUCTIVE DATA **
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 2300 mg/kg
- SEX/DURATION :
- male 71 day(s) pre-mating female 2 week(s) pre-mating - 7 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)
- REFERENCE :
- OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 42,167,1991
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 275 mg/kg
- SEX/DURATION :
- female 7-17 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4 per # born alive)
- REFERENCE :
- OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 42,167,1991
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 260 mg/kg
- SEX/DURATION :
- female 17-21 day(s) after conception lactating female 21 day(s) post-birth
- TOXIC EFFECTS :
- Reproductive - Maternal Effects - parturition Reproductive - Effects on Newborn - live birth index (measured after birth) Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4 per # born alive)
- REFERENCE :
- OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 42,167,1991
苯磺酸氨氯地平安全信息
[ 符号 ]:
GHS07
[ 信号词 ]:
Warning
[ 危害声明 ]:
H302
[ 警示性声明 ]:
P301 + P312 + P330
[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Faceshields;Gloves
[ 危害码 (欧洲) ]:
Xn: Harmful;
[ 风险声明 (欧洲) ]:
R22
[ 安全声明 (欧洲) ]:
26-36
[ 危险品运输编码 ]:
NONH for all modes of transport
[ WGK德国 ]:
3
[ RTECS号 ]:
US7967700
[ 海关编码 ]:
2933990090
苯磺酸氨氯地平合成路线
苯磺酸氨氯地平上下游产品
苯磺酸氨氯地平上游产品
苯磺酸氨氯地平下游产品
苯磺酸氨氯地平制备
1. N-(2-羟乙基)邻苯二甲酸亚酰胺的制备
在反应瓶中加入邻苯二甲酸酐14.8g(0.1mol)和DMF100ml,搅拌升温至50ºC,滴加乙醇胺6.1g(0.1mol)滴毕,升温至95ºC搅拌反应6h.冷却,过滤,水洗,干燥,得白色晶体N-(2-羟乙基)邻苯二甲酸亚酰胺17.6g,收率95.3%mp126.8~128.0ºC.
2. 4-[(2-邻苯二甲酰亚胺)乙氧基]乙酰乙酸乙酯的制备
在反应瓶中加入N-(2-羟乙基)邻苯二甲酸亚酰胺19.5g(0.1mol)和THF60ml,搅拌溶解,降温至10ºC以下#加入NaH8g(0.2mol)搅拌30min.缓慢加入4-氯乙酰乙酸乙酯16.5g(0.1mol),加毕#逐渐升温至40ºC,TLC跟踪反应终点.用冷却的2mol/L盐酸调反应液pH6~7,静置,分出水相,常压蒸出THF回收,用乙酸乙酯(30ml×2)提取,合并提取液和有机相,饱和食盐水洗,无水MgSO4干燥,减压浓缩,得黄色油状物4-[(2-邻苯二甲酰亚胺)乙氧基]乙酰乙酸乙酯32.2g,收率75.8%,含量>75%(HPLC法).
3. 3-氨基-4-[(2-邻苯二甲酰亚胺)乙氧基]-2-丁烯酸乙酯的制备
在反应瓶中加入4-[(2-邻苯二甲酰亚胺)乙氧基]乙酰乙酸乙酯38.3g(90mmol)、乙酸铵8g(0.1mol)、乙醇80ml,搅拌回流反应1h.浓缩回收乙醇,浓缩物加乙酸乙酯100ml溶解,水(60ml×2)洗,减压蒸馏,得浅黄色液体3-氨基-4-[(2-邻苯二甲酰亚胺)乙氧基]-2-丁烯酸乙酯34.7g,收率90.1%,含量>75%(HPLC法).
4. 4-[(2-氯苯基)-3-乙氧羰基]-5-甲氧羰基-6-甲基-2-(2-邻苯二甲酰亚胺)甲基-1,4-二氯吡啶的制备
在反应瓶中加入3-氨基-4-[(2-邻苯二甲酰亚胺)乙氧基]-2-丁烯酸乙酯42.4g(0.1mol)、2-乙氧羰基-3-(2-氯苯基)丙烯酸甲酯23.9g(0.1mol)和乙酸200ml,搅拌回流20h.冷却,得黄色油状物,静置冷却,析出结晶,过滤,干燥,得白色晶体4-[(2-氯苯基)-3-乙氧羰基]-5-甲氧羰基-6-甲基-2-(2-邻苯二甲酰亚胺)甲基-1,4-二氯吡啶53.9g,收率74.5%,mp145~147ºC.
5. 2-[(2-氨基乙氧基)甲基]-4-(2-氯苯基)-3-乙氧羰基-5-甲氧羰基-6-甲基-1,4-二氢吡啶(氨氯地平)的制备
在反应瓶中加入乙醇150ml、4-[(2-氯苯基)-3-乙氧羰基]-5-甲氧羰基-6-甲基-2-(2-邻苯二甲酰亚胺)甲基-1,4-二氯吡啶53.8g(0.10mol)、17mol/L水合肼7.0ml,搅拌回流3h.冷却,过滤,乙酸乙酯重结晶,干燥,得浅黄色固体2-[(2-氨基乙氧基)甲基]-4-(2-氯苯基)-3-乙氧羰基-5-甲氧羰基-6-甲基-1,4-二氢吡啶(氨氯地平)38g,收率93%,mp177~179ºC.
6. 苯磺酸氨氯地平的合成
在反应瓶中加入无水乙醇150ml和2-[(2-氨基乙氧基)甲基]-4-(2-氯苯基)-3-乙氧羰基-5-甲氧羰基-6-甲基-1,4-二氢吡啶(氨氯地平)40.9g(0.1mol),搅拌降温至15 ºC以下,加入苯磺酸19.8g(0.125mol),于室温搅拌5h.过滤,滤饼用乙醇洗,干燥,得苯磺酸氨氯地平52.4g,收率92.5%,mp199~201ºC,含量≥99.0%(HPLC法).
苯磺酸氨氯地平海关
[ 海关编码 ]: 2933990090
[ 中文概述 ]:
2933990090. 其他仅含氮杂原子的杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%
[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期
[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%
苯磺酸氨氯地平文献
Br. J. Pharmacol. 171(22) , 5076-92, (2014)
Previously, a systems pharmacology model was developed characterizing drug effects on the interrelationship between mean arterial pressure (MAP), cardiac output (CO) and total peripheral resistance (T...
[Hypertension. Goal: achieving target blood pressure with only 1 pill daily].MMW Fortschr. Med. 155(6) , 66-7, (2013)
Comparative study between derivative spectrophotometry and multivariate calibration as analytical tools applied for the simultaneous quantitation of Amlodipine, Valsartan and Hydrochlorothiazide.
Spectrochim. Acta. A. Mol. Biomol. Spectrosc. 113 , 215-23, (2013)
Four simple, accurate and specific methods were developed and validated for the simultaneous estimation of Amlodipine (AML), Valsartan (VAL) and Hydrochlorothiazide (HCT) in commercial tablets. The de...
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苯磺酸氨氯地平相关知识
2018-12-24 17:57:26
导读：苯磺酸氨氯地平，商品名络活喜、苯磺酸氨氯地平片。1.高血压（单独或与其他药物合并使用）。 2.心绞痛：尤其自发性心绞痛（单独或与其他药物合并使用）。本药品被归类到心绞痛等药品分类。【药品名称】 通用名称：苯磺酸氨氯地平片 商品名称：苯磺酸氨氯地平片(络活喜) 英文名称：Amlodipi...
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标题：苯磺酸氨氯地平_MSDS_用途_密度_CAS号【111470-99-6】_化源网 地址：https://m.chemsrc.com/mip/cas/111470-99-6_1084283.html