洛开酰胺
洛开酰胺用途
抗心律失常药，兼有局麻作用。用于室性心律失常，室性早搏、复发性室心动过速，也用于心房性早搏、室上性心动过速、顽固性心律失常。
洛开酰胺名称
[ CAS 号 ]:
59729-31-6
[ 中文名 ]:
洛开酰胺
[ 英文名 ]:
Lorcainide
[中文别名 ]:
[英文别名 ]:
- Lorcainidum [INN-Latin]
- LORCAINIDE
- Lorcainida [INN-Spanish]
- Lorcainide [INN:BAN]
- lorcainid
洛开酰胺物理化学性质
[ 密度 ]:
1.161g/cm3
[ 沸点 ]:
503ºC at 760 mmHg
[ 分子式 ]:
C22H27ClN2O
[ 分子量 ]:
370.91600
[ 闪点 ]:
258ºC
[ 精确质量 ]:
370.18100
[ PSA ]:
23.55000
[ LogP ]:
4.72640
[ 折射率 ]:
1.594
[ 储存条件 ]:
2-8°C
洛开酰胺毒性和生态
CHEMICAL IDENTIFICATION
- RTECS NUMBER :
- CY1483600
- CHEMICAL NAME :
- Benzeneacetamide, N-(4-chlorophenyl)-N-(1-(1-methylethyl)-4-piperidinyl )-
- CAS REGISTRY NUMBER :
- 59729-31-6
- BEILSTEIN REFERENCE NO. :
- 0497568
- LAST UPDATED :
- 199612
- DATA ITEMS CITED :
- 5
- MOLECULAR FORMULA :
- C22-H27-Cl-N2-O
- MOLECULAR WEIGHT :
- 370.96
HEALTH HAZARD DATA
ACUTE TOXICITY DATA
- TYPE OF TEST :
- LDLo - Lowest published lethal dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Human - woman
- DOSE/DURATION :
- 50 mg/kg
- TOXIC EFFECTS :
- Behavioral - convulsions or effect on seizure threshold Behavioral - coma Cardiac - pulse rate
- REFERENCE :
- JTCTDW Journal of Toxicology, Clinical Toxicology. (Marcel Dekker, 270 Madison Ave., New York, NY 10016) V.19- 1982- Volume(issue)/page/year: 33,157,1995
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 395 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- RMISDU International Congress and Symposium Series - Royal Society of Medicine Services Limited. (Royal Society of Medicine Services Ltd., 7E. 60th St., New York, NY 10022) No.1- 1978- Volume(issue)/page/year: 49,23,1981
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 18600 ug/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- RMISDU International Congress and Symposium Series - Royal Society of Medicine Services Limited. (Royal Society of Medicine Services Ltd., 7E. 60th St., New York, NY 10022) No.1- 1978- Volume(issue)/page/year: 49,23,1981
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 483 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- RMISDU International Congress and Symposium Series - Royal Society of Medicine Services Limited. (Royal Society of Medicine Services Ltd., 7E. 60th St., New York, NY 10022) No.1- 1978- Volume(issue)/page/year: 49,23,1981
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 18800 ug/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- RMISDU International Congress and Symposium Series - Royal Society of Medicine Services Limited. (Royal Society of Medicine Services Ltd., 7E. 60th St., New York, NY 10022) No.1- 1978- Volume(issue)/page/year: 49,23,1981
洛开酰胺安全信息
[ 危害码 (欧洲) ]:
Xn
[ 安全声明 (欧洲) ]:
26-36/37
洛开酰胺制备
丙烯酸酯和异丙胺在盐类催化剂存在下，室温搅拌，再缓慢升至100-110℃保温。减压蒸出丙烯酸甲酯，收集131～135℃/1.47kPa的馏分，得N，N双(2-甲氧羰基乙基)异丙胺，收率83.5%。将其和固体甲醇钠及无水甲苯，在100-105℃搅拌。蒸出80℃以下的馏分，加入无水甲苯，回流。放冷，加入冰醋酸和水，分出甲苯层，水层用甲苯提取。用浓盐酸提取甲苯层，所有酸液合并，在110℃脱羧反应。经处理后得N-异丙基-4-哌啶酮，收率33%。该哌啶酮、对氯苯胺、对甲苯磺酸和甲苯，回流分水。收集178～180℃/1.47kPa馏分，得1-异丙基-4-(对氯苯基亚氨基)哌啶，收率83%。该哌啶溶于甲醇，分批加入硼氢化钾，回流得1-异丙基-4-(对氯苯氨基)哌啶的氯仿溶液；该氯仿溶液和苯乙酰氯，回流，盐酸酸化至Ph=3。粗品用异丙醇-丙酮混合溶剂重结晶，得劳卡尼，二步收率63.6%，熔点263～265℃。
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