乙吗噻嗪
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- CAS号:
- 31883-05-3
- 英文名:
- Moricizine
- 英文别名:
- Moricizin;Moricizine;TIMTEC-BB SBB005991;Ethmozin:Moricizine;Ethyl (10-(3-Morpholinopropanoyl)-10H-phenothiazin-2-yl)carbaMate;ethyl N-[10-(3-morpholin-4-ylpropanoyl)phenothiazin-2-yl]carbamate;10-(3-Morpholinopropionyl)phenothiazine-2-carbamic acid ethyl ester;N-[10-(3-morpholinopropanoyl)phenothiazin-2-yl]carbamic acid ethyl ester;N-[10-(3-Morpholinopropionyl)-10H-phenothiazin-2-yl]carbamic acid ethyl ester;10-(3-Morpholinopropionyl)-10H-phenothiazin-2-yl carbaminoic acid, ethyl ester
- 中文名:
- 乙吗噻嗪
- 中文别名:
- 安脉静;乙吗噻嗪;吗拉西嗪;安他脉静;莫瑞西嗪;盐酸莫雷西嗪;化合物 T16127;10-(3-吗啉基丙酰基)吩噻嗪-2-氨基甲酸乙酯
- CBNumber:
- CB4493310
- 分子式:
- C22H25N3O4S
- 分子量:
- 427.52
- MOL File:
- 31883-05-3.mol
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乙吗噻嗪化学性质
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熔点:
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156-157°
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沸点:
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625.0±55.0 °C(Predicted)
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密度:
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1.315±0.06 g/cm3(Predicted)
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储存条件:
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-20°C Freezer, Under inert atmosphere
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溶解度:
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Chloroform (Slightly), Methanol (Very Slightly)
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酸度系数(pKa):
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6.4(at 25℃)
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形态:
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Solid
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颜色:
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Pale Orange to Light Orange
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乙吗噻嗪性质、用途与生产工艺
Moricizine (Moracizine) 是吩噻嗪衍生物,可以抑制跨心肌细胞膜的快速内向钠电流 (INa)。Moricizine 是一种抗心律不齐的药物,具有用于室性心动过速的潜力。
Moricizine (Moracizine) induces the tonic block of INa with the apparent dissociation constant (Kd,app) of 6.3 microM at -100 mV and 99.3 microM at -140 mV. Moricizine at 30 microM shifts the h infinity curve to the hyperpolarizing direction by 8.6 +/- 2.4 mV. Moricizine also produces the phasic block of INa, which is enhanced with the increase in the duration of train pulses, and is more prominent with a holding potential (HP) of -100 mV than with an HP of -140 mV. Moricizine exerts an antiarrhythmic action on atrial myocytes, as well as on ventricular myocytes, by blocking Na+ channels with a high affinity to the inactivated state and a slow dissociation kinetics.
化学性质
结晶性粉末,熔点156--157℃。pKa 6.4。
盐酸莫雷西嗪(Moracizine Hydrochloride):C22H25N3O4S?HCl。[29560-58-5]。从二氯乙烷得白色结晶。溶于水或醇。熔点189"C(分解)。急性毒性LD
50小鼠,大鼠(mg/kg):36,12静脉注射。急性毒性LD50小鼠(mg/kg):131腹腔注射。
用途
吩噻嗪衍生物,钠通道阻滞剂,并有局麻活性。抗心律失常药。用于心绞痛、高血压及冠心病等患者的心律失常。
用途
广谱抗心律失常药。
生产方法
往10g(0.035mo1)吩噻嗪-2-氨基甲酸乙酯溶于30ml无水甲苯的溶液中,滴加5.3g(0.042mo1)3-氯丙酰氯,在110~120℃回流4h,加入活性炭进行热过滤,然后冷却至室温。过滤析出的沉淀,得10.2g 10-(3-氯丙酰基)吩噻嗪-2-氨基甲酸乙酯,收率77.5%,熔点169-170℃。
10.2g上面得到的酯化合物溶于50ml甲苯,加入4.72g吗啉,在110~120℃回流3h。过滤除去沉淀出的吗啉盐酸盐,滤液用水洗以除去过剩的吗啉,然后用稀盐酸酸化至Ph值为3。分出酸性水层,用活性炭处理后,再碱化至Ph值为8-9。即得莫雷西嗪,熔点156-157℃。
上面得到的莫雷西嗪用甲苯萃取,萃取液用无水硫酸镁干燥。往该无水甲苯溶液中,加入氯化氢的无水乙醚溶液,直至盐酸莫瑞西嗪完全沉淀出来。该沉淀用二氯甲烷重结晶,得9.35g盐酸莫雷西嗪,收率76.2%,熔点189℃(分解)。
乙吗噻嗪
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31883-05-3, 乙吗噻嗪 相关搜索:
- API
- 生物化工
- 药物
- 心脑血管药物
- 抗心律失常药
- C22H25N3O4S
- 化合物 T16127
- 盐酸莫雷西嗪
- 乙吗噻嗪
- 吗拉西嗪
- 安他脉静
- 安脉静
- 10-(3-吗啉基丙酰基)吩噻嗪-2-氨基甲酸乙酯
- 莫瑞西嗪
- 31883-05-3
- Carbamic acid, N-[10-[3-(4-morpholinyl)-1-oxopropyl]-10H-phenothiazin-2-yl]-, ethyl ester
- Ethyl (10-(3-Morpholinopropanoyl)-10H-phenothiazin-2-yl)carbaMate
- N-[10-(3-morpholinopropanoyl)phenothiazin-2-yl]carbamic acid ethyl ester
- ethyl N-[10-(3-morpholin-4-ylpropanoyl)phenothiazin-2-yl]carbamate
- N-[10-(3-Morpholinopropionyl)-10H-phenothiazin-2-yl]carbamic acid ethyl ester
- Ethmozin:Moricizine
- 10-(3-Morpholinopropionyl)phenothiazine-2-carbamic acid ethyl ester
- 10-(3-Morpholinopropionyl)-10H-phenothiazin-2-yl carbaminoic acid, ethyl ester
- Moricizin
- Moricizine
- CARBAMIC ACID, [10-[3-(4-MORPHOLINYL)-1-OXOPROPYL]-10H-PHENOTHIAZIN-2-YL]-, ETHYL ESTER
- TIMTEC-BB SBB005991