群多普利
群多普利用途
群多普利名称
[ CAS 号 ]:
87679-37-6
[ 中文名 ]:
群多普利
[ 英文名 ]:
Trandolapril
[中文别名 ]:
[英文别名 ]:
- Trandolaprilum [Latin]
- Preran
- Trandolaprilum
- Trandolapril
- Gopten
- Mavik
- Odrik
- Udrik
- MFCD00865776
- Odric
群多普利生物活性
[ 描述 ]:
[ 相关类别 ]:
[参考文献]
[相关活性小分子]
群多普利物理化学性质
[ 密度 ]:
1.2±0.1 g/cm3
[ 沸点 ]:
626.0±55.0 °C at 760 mmHg
[ 熔点 ]:
122-123°C
[ 分子式 ]:
C24H34N2O5
[ 分子量 ]:
430.537
[ 闪点 ]:
332.4±31.5 °C
[ 精确质量 ]:
430.246765
[ PSA ]:
95.94000
[ LogP ]:
3.97
[ 外观性状 ]:
白色粉末
[ 蒸汽压 ]:
0.0±1.9 mmHg at 25°C
[ 折射率 ]:
1.549
[ 储存条件 ]:
Room temp
群多普利MSDS
群多普利毒性和生态
CHEMICAL IDENTIFICATION
- RTECS NUMBER :
- NL6015178
- CHEMICAL NAME :
- 1H-Indole-2-carboxylic acid, octahydro-1-(2-((1-(ethoxycarbonyl)-3-phenylpropyl)am ino)-1- oxopropyl)-, (2S-(1(R*(R*)),2-alpha,3a-alpha,7a-beta))-
- CAS REGISTRY NUMBER :
- 87679-37-6
- LAST UPDATED :
- 199612
- DATA ITEMS CITED :
- 15
- MOLECULAR FORMULA :
- C24-H34-N2-O5
- MOLECULAR WEIGHT :
- 430.60
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 :
- >5 gm/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 27,195,1996
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intraperitoneal
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 1420 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 27,195,1996
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- >2 gm/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 27,195,1996
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 3990 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 27,195,1996
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intraperitoneal
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 1285 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 27,195,1996
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 3 gm/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 27,195,1996
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Mammal - dog
- DOSE/DURATION :
- 2 gm/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 27,195,1996 ** OTHER MULTIPLE DOSE TOXICITY DATA **
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 912 mg/kg/1Y-I
- TOXIC EFFECTS :
- Gastrointestinal - ulceration or bleeding from stomach Kidney, Ureter, Bladder - changes primarily in glomeruli Blood - changes in erythrocyte (RBC) count
- REFERENCE :
- JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku, Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 18(Suppl 1),37,1993
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Mammal - dog
- DOSE/DURATION :
- 2275 mg/kg/91D-I
- TOXIC EFFECTS :
- Kidney, Ureter, Bladder - urine volume increased Blood - normocytic anemia Nutritional and Gross Metabolic - changes in sodium
- REFERENCE :
- JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku, Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 18(Suppl 1),1,1993 ** REPRODUCTIVE DATA **
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 25 gm/kg
- SEX/DURATION :
- male 9 week(s) pre-mating female 2 week(s) pre-mating - 1 week(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 - Specific Developmental Abnormalities - musculoskeletal system
- REFERENCE :
- JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku, Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 18(Suppl 1),93,1993
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 6300 mg/kg
- SEX/DURATION :
- female 14 day(s) pre-mating female 1-7 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Effects on Embryo or Fetus - fetal death
- REFERENCE :
- JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku, Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 18(Suppl 1),93,1993
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 3300 mg/kg
- SEX/DURATION :
- female 7-17 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Specific Developmental Abnormalities - hepatobiliary system Reproductive - Effects on Newborn - physical
- REFERENCE :
- JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku, Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 19(Suppl 1),107,1993
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 750 mg/kg
- SEX/DURATION :
- female 17-20 day(s) after conception lactating female 21 day(s) post-birth
- TOXIC EFFECTS :
- Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4 per # born alive) Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)
- REFERENCE :
- JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku, Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 18(Suppl 1),133,1993
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 330 mg/kg
- SEX/DURATION :
- female 7-17 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Specific Developmental Abnormalities - musculoskeletal system
- REFERENCE :
- JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku, Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 18(Suppl 1),107,1993
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 780 mg/kg
- SEX/DURATION :
- female 17-21 day(s) after conception lactating female 1-21 day(s) post-birth
- TOXIC EFFECTS :
- Reproductive - Effects on Newborn - behavioral Reproductive - Effects on Newborn - physical
- REFERENCE :
- JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku, Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 18(Suppl 1),133,1993
群多普利安全信息
[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
[ 危险品运输编码 ]:
NONH for all modes of transport
[ RTECS号 ]:
NL6015178
群多普利合成路线
群多普利上下游产品
群多普利上游产品
群多普利下游产品
群多普利制备
1. 3-氯-N-乙酰丙氨酸甲酯的制备
在反应瓶中加入3-氯丙氨酸甲酯盐酸盐181g91.04mol)、乙酰氯163.9g(2.08mol)和无水甲苯1500ml,搅拌加热至回流,回流反应5h直至反应混合物成清澈溶液.反应毕将反应液浓缩至干,剩余物用乙酸乙酯/石油醚混合溶剂重结晶,得3-氯-N-乙酰丙氨酸甲酯170g,收率91%,mp104ºC.
2. 3-(2-氧代环己基)-N-乙酰丙氨酸甲酯的制备
在反应瓶中加入上步制备的化合物3-氯-N-乙酰丙氨酸甲酯160g(0.89mol)、1-吡咯基环己烷171.9g(1.12mol) 和无水DMF1200ml,混合均匀后,将该混合物于20~25ºC放置3天.反应溶液在高真空下浓缩,剩余物中加水600ml后,用浓盐酸调至pH2.水层用乙酸乙酯提取,合并有机相,用无水Na2SO4干燥,过滤,滤液浓缩得油状物3-(2-氧代环己基)-N-乙酰丙氨酸甲酯粗品220g,收率>100%.直接用于下步反应.
3. 3,3a,4,5,6,7-2H-六氢吲哚-2-羧酸盐酸盐的制备
在反应瓶中加入上步制备的化合物3-(2-氧代环己基)-N-乙酰丙氨酸甲酯220g(约0.90mol)(粗品)和2mol/L盐酸1000ml,搅拌加热至沸回流,搅拌回流反应2H.将反应混合物用乙酸乙酯提取,水溶液相浓缩,残留量的水加入甲苯三次,真空共沸蒸馏除去,得黄色油状物3,3a,4,5,6,7-2H-六氢吲哚-2-羧酸盐酸盐210g,收率>100%,该品冷却静置可结晶固化.
4. DL-2β,3αβ,7αa-八氢吲哚-2-羧酸的制备
在氢化反应瓶中加入上步制备的化合物3,3a,4,5,6,7-2H-六氢吲哚-2-羧酸盐酸盐128g(约0.63mol)、冰乙酸700ml和Pd/C(10%)4g,搅拌下用N2置换瓶中空气3次,用H2置换N2后,通H2常压室温氢化反应.反应毕,过滤掉催化剂,滤液浓缩至干,剩余物加热乙醇500ml溶解,将溶液冷却至-20ºC,化合物DL-2β,3αβ,7αa-八氢吲哚-2-羧酸的异构体(2αβ,3αβ, 7αβ-八氢吲哚羧酸)被沉淀出来,分离后的溶液经浓缩后用异丙醇析晶,过滤,得无色晶体DL-2β,3αβ,7αa-八氢吲哚-2-羧酸280g,mp280ºC
5. DL-2β,3αβ,7αa-八氢吲哚-2-羧酸苄酯盐酸盐的制备
在反应瓶中加入苯甲醇14ml(14.58g,134.84mmol)和亚硫酰氯(SOCl2)1.41ml(2.29g,19.27mmol)冷却至-5ºC~0ºC,再在搅拌下于-10ºC~0ºC加入上步制备的化合物DL-2β,3αβ,7αa-八氢吲哚-2-羧酸1.4g(8.28mmol),加毕,将混合物于0ºC搅拌反应1h.于20~25ºC静置过夜.于50ºC将反应液中苄醇(苯甲醇)在高真空下蒸馏干净,剩余物加二异丙醚捣碎研磨,过滤,得DL-2β,3αβ,7αa-八氢吲哚-2-羧酸苄酯盐酸盐2.5g,收率>100%,该产物为无色晶体(仍系粗品),mp154ºC.可直接用于下步反应.
6. N-(1S-乙氧羰基-3-苯丙基)-S-丙氨酰-2β,3αβ,7αa-八氢吲哚-2-羧酸苄酯的制备
在反应瓶中加入N-(1S-乙氧羰基-3-苯丙基)-S-丙氨酸2.16g(7.74mmol)和无水DMF8.6ml,搅拌悬浮,往该悬浮液加入1-羟基苯并三唑1.06g(7.85mol)、上步制备的化合物DL-2β,3αβ,7αa-八氢吲哚-2-羧酸苄酯盐酸盐2.2g(7.45mol)和N-乙基吗啉1.08ml,搅拌混合,再加入二环己基碳化二亚胺(DCC)1.7g(加DCC时控制内温为0ºC),加毕,在20~25ºC搅拌反应3.5h.反应混合物用乙酸乙酯200ml稀释,将产生的二环己基脲沉淀过滤掉,滤液减压浓缩蒸除溶剂,剩余物加入乙醚溶解,溶液用饱和NaHCO3水溶液洗涤2次,无水Na2SO4干燥,过滤,滤液浓缩后剩余物用硅胶柱色谱分离纯化[洗脱剂:乙酸乙酯/环己烷],经后处理得两部分淡黄色油状物(比率为1:1),各含目的化合物N-(1S-乙氧羰基-3-苯丙基)-S-丙氨酰-2β,3αβ,7αa-八氢吲哚-2-羧酸苄酯的一个异构体[即(2R,3αR, 7αS)-N-(1S-乙氧羰基-3-苯丙基)-S-丙氨酰-2β,3αβ,7αa-八氢吲哚-2-羧酸苄酯和(2S,3αS,7αR)- N-(1S-乙氧羰基-3-苯丙基)-S-丙氨酰-2β,3αβ,7αa-八氢吲哚-2-羧酸苄酯.
7. (2S,3αR,7αS)-1-[(2S)-2-[[(1S)-1-(乙氧羰基)-3-苯基丙基]氨基]-1-氧代丙基]八氢-1H-吲哚-2-羧酸(群多普利)的合成
在氢化反应瓶中加入(2S,3αS,7αR)N-(1S-乙氧羰基-3-苯丙基)-S-丙氨酰-2β,3αβ,7αa-八氢吲哚-2-羧酸苄酯1.7g(3.26mol)、无水乙醇60ml和10%Pd/C催化剂200mg,用N2置换瓶中空气3次#用H2置换N2 3次,于25ºC常压通H2反应2h(搅拌下).反应毕,过滤掉催化剂,滤液浓缩蒸除溶剂,得无色泡沫状物(2S,3αR,7αS)-1-[(2S)-2-[[(1S)-1-(乙氧羰基)-3-苯基丙基]氨基]-1-氧代丙基]八氢-1H-吲哚-2-羧酸(群多普利)1.2g,收率85.7%(将该泡沫状目的物制成盐酸盐可得无色无定形粉末).
群多普利文献
J. Emerg. Med. 40(3) , 291-5, (2011)
Patients with fixed-dose combination product overdoses involving verapamil and trandolapril may present differently than sole calcium channel blocker (CCB) or angiotensin-converting enzyme inhibitor (...
Dual therapy versus monotherapy of trandolapril and telmisartan on diabetic nephropathy in experimentally induced type 2 diabetes mellitus rats.J. Renin Angiotensin Aldosterone Syst. 12(3) , 169-75, (2011)
To investigate the combination of telmisartan with trandolapril therapy versus monotherapy of trandolapril and telmisartan on diabetic nephropathy in type 2 diabetes mellitus rats.Neonatal rats (2 day...
Tarka® overdose in a young child.Hum. Exp. Toxicol. 30(9) , 1392-8, (2011)
Tarka® is a combination antihypertensive medication composed of verapamil hydrochloride and trandolapril. A 3.5-year-old female was brought to our hospital due to a sleepy condition 7 hours after an a...
推荐生产厂家/供应商：
公司名：上海化源世纪贸易有限公司
区域：上海市普陀区
价格：
联系人：徐经理
产品详情：群多普利
公司名：上海源溪生物科技有限公司
区域：上海市浦东新区
价格：
￥需询单/1g
联系人：赖经理
产品详情：Trandolapril
公司名：上海脉铂医药科技有限公司
区域：上海市嘉定区
价格：
￥689.0/10mg
￥2989.0/50mg
￥需询单/1g
￥需询单/1g
联系人：李先生
产品详情：Trandolapril
公司名：上海创赛科技有限公司
区域：上海市嘉定区
价格：
￥3586.0/50mg
￥906.0/10mg
￥686.0/10mg
￥2940.0/50mg
联系人：夏言
产品详情：[Perfemiker]Trandolapril,≥98%
公司名：上海阿拉丁生化科技股份有限公司
区域：上海市浦东新区
价格：
￥1071.9/25mg
￥308.9/5mg
￥514.9/1ml
￥2986.9/100mg
联系人：阿拉丁
产品详情：Trandolapril
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相关化合物
【群多普利】化源网提供群多普利CAS号87679-37-6，群多普利MSDS及其说明、性质、英文名、生产厂家、作用/用途、分子量、密度、沸点、熔点、结构式等。CAS号查询群多普利上化源网，专业又轻松。>>电脑版：群多普利
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