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索他洛尔

索他洛尔用途

用作降血压药

索他洛尔名称

[ CAS 号 ]:
3930-20-9

[ 中文名 ]:
索他洛尔

[ 英文名 ]:
Sotalol

[中文别名 ]:

[英文别名 ]:

MFCD00242936
Sotalol

索他洛尔物理化学性质

[ 密度 ]:
1.239 g/cm3

[ 沸点 ]:
443.3ºC at 760 mmHg

[ 分子式 ]:
C₁₂H₂₀N₂O₃S

[ 分子量 ]:
272.36400

[ 闪点 ]:
221.9ºC

[ 精确质量 ]:
272.11900

[ PSA ]:
86.81000

[ LogP ]:
2.63420

[ 外观性状 ]:
白色结晶

[ 折射率 ]:
1.57

索他洛尔毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: PB0825900

CHEMICAL NAME :: Methanesulfonanilide, 4'-(1-hydroxy-2-(isopropylamino)ethyl)-

CAS REGISTRY NUMBER :: 3930-20-9

LAST UPDATED :: 199806

DATA ITEMS CITED :: 7

MOLECULAR FORMULA :: C12-H20-N2-O3-S

MOLECULAR WEIGHT :: 272.40

WISWESSER LINE NOTATION :: WS1&MR DYQ1MY1&1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 118 mg/kg/4W-I

TOXIC EFFECTS :: Cardiac - EKG changes not diagnostic of specified effects Cardiac - pulse rate Cardiac - change in rate

REFERENCE :: PGMJAO Postgraduate Medical Journal. (Blackwell Scientific Pub. Ltd., POB 88, Oxford, UK) V.1- 1925- Volume(issue)/page/year: 68,289,1992

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 3429 ug/kg/2D-I

TOXIC EFFECTS :: Cardiac - pulse rate increase, without fall in BP Cardiac - pulse rate Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: ANZJB8 Australian and New Zealand Journal of Medicine. (Modern Medicine of Australia Pty., Ltd., 100 Pacific Highway, North Sydney, 2060, Australia) V.1- 1971- Volume(issue)/page/year: 24,319,1994

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 288 mg/kg

TOXIC EFFECTS :: Behavioral - coma Cardiac - change in rate Vascular - BP lowering not characterized in autonomic section

REFERENCE :: JTCTDW Journal of Toxicology, Clinical Toxicology. (Marcel Dekker, 270 Madison Ave., New York, NY 10016) V.19- 1982- Volume(issue)/page/year: 26,389,1988

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 14 mg/kg/3D-I

TOXIC EFFECTS :: Cardiac - pulse rate increase, without fall in BP Cardiac - pulse rate Vascular - BP lowering not characterized in autonomic section

REFERENCE :: ANZJB8 Australian and New Zealand Journal of Medicine. (Modern Medicine of Australia Pty., Ltd., 100 Pacific Highway, North Sydney, 2060, Australia) V.1- 1971- Volume(issue)/page/year: 24,319,1994

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Multiple routes

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 100 mg/kg/2W-I

TOXIC EFFECTS :: Cardiac - other changes

REFERENCE :: AHJOA2 American Heart Journal. (C.V. Mosby Co., 11830 Westline Industrial Dr., St. Louis, MO 63146) V.1- 1925- Volume(issue)/page/year: 107,179,1984

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 790 mg/kg

TOXIC EFFECTS :: Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: PJPPAA Polish Journal of Pharmacology and Pharmacy. (ARS Polona, POB 1001, 00-068 Warsaw 1, Poland) V.25- 1973- Volume(issue)/page/year: 25,145,1973

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 113 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: USXXAM United States Patent Document. (U.S. Patent Office, Box 9, Washington, DC 20231) Volume(issue)/page/year: #5179095

索他洛尔安全信息

[ 危害码 (欧洲) ]:
Xi:Irritant;

[ 风险声明 (欧洲) ]:
R36/37/38

[ 安全声明 (欧洲) ]:
S26-S36

[ 海关编码 ]:
2935009090

索他洛尔合成路线

详细合成路线

索他洛尔上下游产品

索他洛尔上游产品

索他洛尔下游产品

索他洛尔制备

在冰浴和搅拌下，将甲磺酰氯滴加到苯胺、三乙胺和乙醇的溶液中，然后室温搅拌。过滤，滤液浓缩，结晶后，用乙醇重结晶，烘干得甲磺酰苯胺。在冰浴和搅拌下，在甲磺酰苯胺、溴乙酰溴和二硫化碳的溶液中，加入无水三氯化铝，回流。经过滤、重结晶，将得到的化合物加入异丙胺的甲醇溶液中，反应。减压浓缩，加丙酮，通入氯化氢至pH值为2.将反应液处理，得到的化合物溶于甲醇，加Pd-C,通入氢气反应，反应完毕后，过滤，滤液浓缩至干，加甲醇热至全溶，活性炭脱色。冷却，过滤得白色的盐酸索他洛尔。

索他洛尔海关

[ 海关编码 ]: 2935009090

[ 中文概述 ]:
2935009090 其他磺（酰）胺. 增值税率:17.0% 退税率:9.0% 监管条件:无最惠国关税:6.5% 普通关税:35.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2935009090 other sulphonamides VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:35.0%