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519-98-2

中文名称 4-(甲氨基)安替比林
英文名称 1,2-dihydro-1,5-dimethyl-4-(methylamino)-2-phenyl-3H-pyrazol-3-one
CAS 519-98-2
分子式 C12H15N3O
分子量 217.27
MOL 文件 519-98-2.mol
更新日期 2024/07/07 17:01:58
519-98-2 结构式 519-98-2 结构式

基本信息

中文别名
安乃近杂质3
咪达唑仑杂质C
4-单甲基氨基安替比林
4-(甲氨基)安替比林
4-(甲基氨基)安替比林
安替比林,4-(甲基氨基)-
METAMIZOLE 杂质C
1,5-二甲基-4-甲基氨基-2-苯基-3-吡唑酮
1,5-二甲基-4-甲基氨基-2-苯基吡唑-3-酮
1,5-二甲基-4-甲基氨基-2-苯基-吡唑-3-酮
英文别名
N-Methy
Noraminopyrine
noramidopyrine
Methylaminophenazone
Methylaminoantipyrine
Metamizole Impurity C
N-Methylaminophenazone
4-Methylaminophenazone
Monomethylaminoantipyrine
4-(Methylamino)-antipyrine
所属类别
医药中间体:原料药中间体

物理化学性质

外观性状油状液体。
熔点50-53°C
沸点324.5±45.0 °C(Predicted)
密度1.20±0.1 g/cm3 (20 ºC 760 Torr)
储存条件-20°C冷冻
溶解度可溶于氯仿(少许)、乙酸乙酯(少许)、甲醇(少许)
酸度系数(pKa)4.76±0.20(Predicted)
形态固体
颜色淡黄色至棕色

安全数据

危险性符号(GHS)
GHS07
警示词警告
危险性描述H302
危险等级IRRITANT
毒性LD50 oral in mouse: 7gm/kg

应用领域

用途1
安乃近的中间体。

制备方法

方法1
用氨基安替比林以甲酸甲酰化,生成4-(甲酰氨基)安替比林,然后以硫酸二甲酯在碱性条件下甲基化,得4-甲酰甲氨基安替比林,将后者以硫酸水解(去除甲酰基)并中和制得该品。

上下游产品信息

下游产品
海藻酸铵

常见问题列表

生物活性
4-Methylamino antipyrine 是一种 Metamizole 的活性代谢产物。Metamizole 是吡唑啉酮类非甾体抗炎药 (NSAID),可抑制 COX。Metamizole 是一种非阿片类镇痛药,可用于疼痛和发烧。4-Methylamino antipyrine 具有止痛,解热和相对较弱的抗炎特性。
靶点

COX

体外研究

Metamizole is a prodrug which, at room temperature and in an atmosphere with oxygen, is spontaneously, nonenzymatically converted to 4-Methylamino antipyrine. Subsequently, the N-methyl side chain of 4-Methylamino antipyrine is oxidized to yield 4-formylaminoantipyrine, which is further converted to 4-aminoantipyrine. Metamizole in aqueous solution and in the presence of oxygen consists of a group of several pyrazolone derivatives of which 4-Methylamino antipyrine is pharmacologically the most important.

体内研究

The aim of this study is to assess the pharmacokinetics of its active metabolites 4-Methylamino antipyrine in male piglets after a single intramuscular injection of Metamizole. Eight healthy male piglets are administered Metamizole (100 mg/kg) intramuscularly. 4-Methylamino antipyrine plasma concentrations are quantitatively detectable from 0.25 to 48 h. The average maximum concentrations of 4-Methylamino antipyrine is of 47.59 mg/mL. The average half-lives is 8.57 h for 4-Methylamino antipyrine.

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