盐酸曲唑酮
盐酸曲唑酮用途
盐酸曲唑酮作用
盐酸曲唑酮名称
[ CAS 号 ]:
25332-39-2
[ 中文名 ]:
盐酸曲唑酮
[ 英文名 ]:
trazodone hydrochloride
[中文别名 ]:
[英文别名 ]:
- trazolan
- AzoNa
- Trittico
- BiMaran
- Trazodone (hydrochloride)
- Mesyrel
- Trazodone HCl
- tombran
- thombran
- MFCD00079603
盐酸曲唑酮生物活性
[ 描述 ]:
[ 相关类别 ]:
[参考文献]
[相关活性小分子]
盐酸曲唑酮物理化学性质
[ 沸点 ]:
528.5ºC at 760 mmHg
[ 熔点 ]:
223ºC
[ 分子式 ]:
C19H23Cl2N5O
[ 分子量 ]:
408.325
[ 闪点 ]:
273.4ºC
[ 精确质量 ]:
407.127960
[ PSA ]:
45.78000
[ LogP ]:
3.16660
[ 外观性状 ]:
powder | off-white
[ 蒸汽压 ]:
2.94E-11mmHg at 25°C
[ 储存条件 ]:
-20°C Freezer
[ 水溶解性 ]:
45% (w/v) aq 2-hydroxypropyl-β-cyclodextrin: 23.3 mg/mL
盐酸曲唑酮MSDS
盐酸曲唑酮毒性和生态
CHEMICAL IDENTIFICATION
- RTECS NUMBER :
- XZ5660000
- CHEMICAL NAME :
- s-Triazolo(4,3-a)pyridin-3(2H)-one, 2-(3-(4-(m-chlorophenyl)-1-piperazinyl)propyl)-, monohydrochloride
- CAS REGISTRY NUMBER :
- 25332-39-2
- LAST UPDATED :
- 199706
- DATA ITEMS CITED :
- 29
- MOLECULAR FORMULA :
- C19-H22-Cl-N5-O.Cl-H
- MOLECULAR WEIGHT :
- 408.37
- WISWESSER LINE NOTATION :
- T56 ANVNNJ C3- AT6N DNTJ DR CG &GH
HEALTH HAZARD DATA
ACUTE TOXICITY DATA
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Human - man
- DOSE/DURATION :
- 5714 ug/kg/4D-I
- TOXIC EFFECTS :
- Behavioral - euphoria Behavioral - excitement
- REFERENCE :
- BJPYAJ British Journal of Psychiatry. (Headley Brothers, Ltd., Ashford, Kent TN24 8HH, UK) V.109- 1963- Volume(issue)/page/year: 158,275,1991
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Human - man
- DOSE/DURATION :
- 43 mg/kg/30D-I
- TOXIC EFFECTS :
- Blood - agranulocytosis Blood - other changes
- REFERENCE :
- AJPSAO American Journal of Psychiatry. (American Psychiatric Assoc., Circulation Dept., 1400 K St., NW, Washington, DC 20005) V.78- 1921- Volume(issue)/page/year: 150,1563,1993
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Human - woman
- DOSE/DURATION :
- 750 ug/kg
- TOXIC EFFECTS :
- Behavioral - hallucinations, distorted perceptions
- REFERENCE :
- AJPSAO American Journal of Psychiatry. (American Psychiatric Assoc., Circulation Dept., 1400 K St., NW, Washington, DC 20005) V.78- 1921- Volume(issue)/page/year: 141,434,1984
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Human - woman
- DOSE/DURATION :
- 720 mg/kg/34W-I
- TOXIC EFFECTS :
- Liver - hepatitis (hepatocellular necrosis), zonal Liver - jaundice (or hyperbilirubinemia) hepatocellular Kidney, Ureter, Bladder - other changes in urine composition
- REFERENCE :
- AIMEAS Annals of Internal Medicine. (American College of Physicians, 4200 Pine St., Philadelphia, PA 19104) V.1- 1927- Volume(issue)/page/year: 118,791,1993
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Human - man
- DOSE/DURATION :
- 46 mg/kg/8D-I
- TOXIC EFFECTS :
- Behavioral - excitement Cardiac - pulse rate increase, without fall in BP Kidney, Ureter, Bladder - urine volume increased
- REFERENCE :
- JCPYDR Journal of Clinical Pyschopharmacology. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1981- Volume(issue)/page/year: 6,117,1986
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Human - man
- DOSE/DURATION :
- 667 ug/kg
- TOXIC EFFECTS :
- Cardiac - cardiomyopathy including infarction
- REFERENCE :
- AJPSAO American Journal of Psychiatry. (American Psychiatric Assoc., Circulation Dept., 1400 K St., NW, Washington, DC 20005) V.78- 1921- Volume(issue)/page/year: 141,1472,1984
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Human - woman
- DOSE/DURATION :
- 80 mg/kg
- TOXIC EFFECTS :
- Behavioral - somnolence (general depressed activity) Vascular - BP lowering not characterized in autonomic section Lungs, Thorax, or Respiration - respiratory depression
- REFERENCE :
- JATOD3 Journal of Analytical Toxicology. (Preston Pub. Inc., POB 48312, Niles, IL 60648) V.1- 1977- Volume(issue)/page/year: 8,91,1984
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 690 mg/kg
- TOXIC EFFECTS :
- Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - cyanosis Gastrointestinal - changes in structure or function of salivary glands
- REFERENCE :
- MPPPBK Modern Problems of Pharmacopsychiatry. (S. Karger AG, Postfach, CH-4009 Basel, Switzerland) V.1- 1968- Volume(issue)/page/year: 9,76,1974
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intraperitoneal
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 178 mg/kg
- TOXIC EFFECTS :
- Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - cyanosis Gastrointestinal - changes in structure or function of salivary glands
- REFERENCE :
- MPPPBK Modern Problems of Pharmacopsychiatry. (S. Karger AG, Postfach, CH-4009 Basel, Switzerland) V.1- 1968- Volume(issue)/page/year: 9,76,1974
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Subcutaneous
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 2729 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: 22,967,1991
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 91 mg/kg
- TOXIC EFFECTS :
- Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - cyanosis Gastrointestinal - changes in structure or function of salivary glands
- REFERENCE :
- MPPPBK Modern Problems of Pharmacopsychiatry. (S. Karger AG, Postfach, CH-4009 Basel, Switzerland) V.1- 1968- Volume(issue)/page/year: 9,76,1974
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 584 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- DDREDK Drug Development Research. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1981- Volume(issue)/page/year: 22,385,1991
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intraperitoneal
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 255 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- JPMSAE Journal of Pharmaceutical Sciences. (American Pharmaceutical Assoc., 2215 Constitution Ave., NW, Washington, DC 20037) V.50- 1961- Volume(issue)/page/year: 81,99,1992
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Subcutaneous
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- >1500 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: 22,967,1991
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 91 mg/kg
- TOXIC EFFECTS :
- Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - cyanosis Gastrointestinal - changes in structure or function of salivary glands
- REFERENCE :
- MPPPBK Modern Problems of Pharmacopsychiatry. (S. Karger AG, Postfach, CH-4009 Basel, Switzerland) V.1- 1968- Volume(issue)/page/year: 9,76,1974
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Mammal - dog
- DOSE/DURATION :
- 500 mg/kg
- TOXIC EFFECTS :
- Behavioral - altered sleep time (including change in righting reflex) Behavioral - convulsions or effect on seizure threshold Behavioral - aggression
- REFERENCE :
- MPPPBK Modern Problems of Pharmacopsychiatry. (S. Karger AG, Postfach, CH-4009 Basel, Switzerland) V.1- 1968- Volume(issue)/page/year: 9,76,1974
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Mammal - dog
- DOSE/DURATION :
- >40 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- MPPPBK Modern Problems of Pharmacopsychiatry. (S. Karger AG, Postfach, CH-4009 Basel, Switzerland) V.1- 1968- Volume(issue)/page/year: 9,76,1974
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Primate - monkey
- DOSE/DURATION :
- 25 mg/kg
- TOXIC EFFECTS :
- Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - cyanosis Gastrointestinal - changes in structure or function of salivary glands
- REFERENCE :
- PBPSDY Pharmacological and Biochemical Properties of Drug Substances. (American Pharmaceutical Assoc., 2215 Constitution Ave., NW, Washington, DC 20037) V.1- 1977- Volume(issue)/page/year: 3,94,1981
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - rabbit
- DOSE/DURATION :
- 560 mg/kg
- TOXIC EFFECTS :
- Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - cyanosis Gastrointestinal - changes in structure or function of salivary glands
- REFERENCE :
- MPPPBK Modern Problems of Pharmacopsychiatry. (S. Karger AG, Postfach, CH-4009 Basel, Switzerland) V.1- 1968- Volume(issue)/page/year: 9,76,1974
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Rodent - rabbit
- DOSE/DURATION :
- 52 mg/kg
- TOXIC EFFECTS :
- Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - cyanosis Gastrointestinal - changes in structure or function of salivary glands
- REFERENCE :
- MPPPBK Modern Problems of Pharmacopsychiatry. (S. Karger AG, Postfach, CH-4009 Basel, Switzerland) V.1- 1968- Volume(issue)/page/year: 9,76,1974 ** OTHER MULTIPLE DOSE TOXICITY DATA **
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 66175 mg/kg/78W-C
- TOXIC EFFECTS :
- Endocrine - changes in adrenal weight Endocrine - changes in thyroid weight Related to Chronic Data - changes in testicular weight
- REFERENCE :
- KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 23,5865,1989
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Mammal - dog
- DOSE/DURATION :
- 2730 mg/kg/13W-I
- TOXIC EFFECTS :
- Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - phosphatases
- REFERENCE :
- YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 17(Suppl 5),S1259,1989 ** REPRODUCTIVE DATA **
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 159 mg/kg
- SEX/DURATION :
- male 7 week(s) pre-mating
- TOXIC EFFECTS :
- Reproductive - Paternal Effects - impotence
- REFERENCE :
- AJPSAO American Journal of Psychiatry. (American Psychiatric Assoc., Circulation Dept., 1400 K St., NW, Washington, DC 20005) V.78- 1921- Volume(issue)/page/year: 140,1256,1983
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 112 mg/kg
- SEX/DURATION :
- male 6 week(s) pre-mating
- TOXIC EFFECTS :
- Reproductive - Paternal Effects - other effects on male
- REFERENCE :
- JCLPDE Journal of Clinical Psychiatry. (Physicians Postgraduate Press, Inc., POB 240008, Memphis, TN 38124) V.39- 1978- Volume(issue)/page/year: 45,232,1984
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 667 ug/kg
- SEX/DURATION :
- male 1 day(s) pre-mating
- TOXIC EFFECTS :
- Reproductive - Paternal Effects - other effects on male
- REFERENCE :
- AJPSAO American Journal of Psychiatry. (American Psychiatric Assoc., Circulation Dept., 1400 K St., NW, Washington, DC 20005) V.78- 1921- Volume(issue)/page/year: 142,142,1985
- 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 - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Effects on Embryo or Fetus - fetal death Reproductive - Specific Developmental Abnormalities - musculoskeletal system
- REFERENCE :
- YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 17(Suppl 5),1283,1989
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 1100 mg/kg
- SEX/DURATION :
- female 7-17 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Effects on Newborn - physical
- REFERENCE :
- YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 17(Suppl 5),1283,1989
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 750 mg/kg
- SEX/DURATION :
- female 7-20 day(s) after conception lactating female 21 day(s) post-birth
- TOXIC EFFECTS :
- Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)
- REFERENCE :
- YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 17(Suppl 5),1301,1989 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X5669 No. of Facilities: 24 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 333 (estimated) No. of Female Employees: 219 (estimated)
盐酸曲唑酮安全信息
[ 符号 ]:
GHS02, GHS06, GHS08
[ 信号词 ]:
Danger
[ 危害声明 ]:
H225-H301 + H311 + H331-H370
[ 警示性声明 ]:
P210-P260-P280-P301 + P310-P311
[ 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) ]:
Xn:Harmful
[ 风险声明 (欧洲) ]:
R22;R40
[ 安全声明 (欧洲) ]:
S22-S36
[ 危险品运输编码 ]:
3249
[ WGK德国 ]:
3
[ RTECS号 ]:
XZ5660000
[ 包装等级 ]:
III
[ 危险类别 ]:
6.1(b)
[ 海关编码 ]:
2933990090
盐酸曲唑酮上下游产品
盐酸曲唑酮上游产品
盐酸曲唑酮下游产品
盐酸曲唑酮制备
1. 吡啶肼的制备
在反应瓶中加入2-氯吡啶3.8g(0.04mol)和水合肼30ml,搅拌回流24h.应液用乙醚(20ml×2)提取,水层浓缩,用乙醚(15ml×6)提取,合并乙醚提取液,水洗,无水Na2SO4干燥,蒸去乙醚,冷却,得白色固体,干燥得吡啶肼2.9g,收率67%,mp50~51ºC.
2. 1,2,4-三唑并-[4,3-a]吡啶-3(2H)-酮制备
在反应瓶中加入吡啶肼1.4g(0.013mol)和脲1.7g(0.03mol),混合,加热熔融,于155~160ºC反应2h.稍冷后加入水30ml,搅拌,抽滤,水洗,干燥得1,2,4-三唑并-[4,3-a]吡啶-3(2H)-酮1.5g,收率86.5%,mp224~226ºC.
3. 盐酸曲唑酮的合成
在反应瓶中加入1,2,4-三唑并-[4,3-a]吡啶-3(2H)-酮1.0g(7.4mmol)、1-(3-氯苯基)-4-(3-氯丙基)哌嗪盐酸盐2.4g(7.4mmol)和乙醇20ml,搅拌下加入NaOH0.6g(0.015mol),搅拌回流30h.热过滤,少量乙醇洗,洗液和滤液合并,减压浓缩至干.剩余物加水10ml,用二氯甲烷(10ml×3) 提取.合并提取液,水洗,无水Na2SO4干燥,过滤,滤液蒸除溶剂,加无水乙醇10ml溶解,通入干燥的HCl气体,产生大量固体,过滤,滤饼用少量无水乙醇洗,用无水乙醇重结晶,得白色固体盐酸曲唑酮2.1g,收率67.5%,mp222~225 ºC.
盐酸曲唑酮海关
[ 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%
盐酸曲唑酮文献
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A 49-year-old man was admitted to this hospital after being found unresponsive outdoors; he was next to a half-filled bottle of cloudy liquid with pill fragments. An electrocardiogram showed a QTc int...
Serotonergic signalling suppresses ataxin 3 aggregation and neurotoxicity in animal models of Machado-Joseph disease.Brain 138 , 3221-37, (2015)
Polyglutamine diseases are a class of dominantly inherited neurodegenerative disorders for which there is no effective treatment. Here we provide evidence that activation of serotonergic signalling is...
Spectroscopic and calorimetric studies on trazodone hydrochloride-phosphatidylcholine liposome interactions in the presence and absence of cholesterol.Biochim. Biophys. Acta 1838(10) , 2369-79, (2014)
The interaction of antidepressant drug trazodone hydrochloride (TRZ) with dipalmitoyl phosphatidylcholine (DPPC) multilamellar liposomes (MLVs) in the presence and absence of cholesterol (CHO) was inv...
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公司名:西安康诺化工有限公司
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