百科

洛伐他汀

洛伐他汀

CAS号：75330-75-5

英文名：lovastatin

分子式

C24H36O5

熔点

175°C

密度

1.12 g/cm3

分子量

404.54

沸点

559.2ºC at 760 mmHg

溶解度

0.0004 mg/mL at 25 ºC

信号词

危险品标志

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化合物简介

An antihypercholesterolemic agent. A fungal metabolite, which is a potent inhibitor of HMG-CoA reductase.

基本信息

中文名称

洛伐他汀

英文名称

lovastatin

中文别名

洛伐司他汀、洛伐它丁、辛伐他汀杂质E

英文别名

LOVASTIN、MEVINOLIN、LOVALIP、mevlor、Lovastatin、Rovacor、MEVACOR、msd803、Sivlor、Paschol

CAS号

75330-75-5

分子式

C24H36O5

分子量

404.54

精确质量

404.256

PSA

72.83

LOGP

4.1955

编号系统

UNII

9LHU78OQFD

物化性质

外观与性状

白色固体

密度

1.12 g/cm3

沸点

559.2ºC at 760 mmHg

熔点

175°C

闪点

185.3ºC

折射率

320 ° (C=0.5, CH3CN)

水溶解性

0.0004 mg/mL at 25 ºC

储存条件

2-8ºC

安全信息

RTECS号

EK7907000

安全说明

S22-S24/25

危险类别码

R36/37/38

WGK Germany

3

海关编码

2932999099

危险品运输编码

3077

危险类别

9

包装等级

III

危险品标志

Xi

生产方法及用途

生产方法

洛伐他汀经发酵得到。可用的菌种有:①Monescus ruber;②Monescus purpureus;③Monescus pilosus;④Aspergillus terreus;⑤Penicillium Citrunum。用Monescus ruber作为菌种时,其培养液为:6%葡萄糖、2.5%胨、0.5%玉米浆、0.5%氯化铵。菌种和培养液一起,在28℃需氧条件下培养10d。过滤取5L滤液,用5L Ph值为3的乙酸乙酯提取。提取液真空浓缩至干,剩余物溶于100ml苯。过滤除去不溶物,滤液用100ml 5%碳酸钠水溶液洗2次,然后和100ml0.2mol/L氢氧化钠溶液一起在室温下搅拌2h。收集水层,用6mol/L盐酸调至Ph=3后,用100ml乙酸乙酯提取2次。提取液合并蒸发至干,得260mg油状物。将该油状物溶于小量苯,得到的结晶再用丙酮和水的混合液重结晶,得87mg无色的洛伐他汀结晶,熔点157～159℃(分解),[α]D23+307.6°(C=1,甲醇)。

用途

心血管系统用药，能阻止动脉硬化的发展、减少心肌梗塞等的发病危险。

合成路线

共找到8条合成路线 >

117020-90-3

洛伐他汀

海关数据

共找到1个国家海关数据 >

国家/地区名称	海关编码	更新时间	操作
中国	2932999099	2019-03	查看

上游原料

共找到25个上游原料 >

4-(叔丁基二甲基甲硅烷氧基)-6-[2-(8-羟基-2,6-二甲基-1,2,6,7,8,8a-六氢萘)-乙基]-四氢吡喃-2-酮

4-(叔丁基二甲基甲硅烷氧基)-6-[2-(8-羟基-2,6-二甲基-1,2,6,7,8,8a-六氢萘)-乙基]-四氢吡喃-2-酮

<4S-<4α,5α(4S*,6R*),6β(1R*,3S*)>>-5-<2-<6-<2-<<(1,1-dimethylethyl)diphenylsilyl>oxy>ethyl>-2,2-dimethyl-1,3-dioxan-4-yl>ethyl>-4-methyl-6-<3-methyl-1-<(triethylsilyl)oxy>-4-pentenyl>-2-cyclohexen-1-one

<4S-<4α,5α(4S*,6R*),6β(1R*,3S*)>>-5-<2-<6-<2-<<(1,1-dimethylethyl)diphenylsilyl>oxy>ethyl>-2,2-dimethyl-1,3-dioxan-4-yl>ethyl>-4-methyl-6-<3-methyl-1-<(triethylsilyl)oxy>-4-pentenyl>-2-cyclohexen-1-one

洛伐他汀钠

洛伐他汀钠

<4R-<4α(4R*,5R*),6α>>-5-<2-<6-<2-<<(1,1-dimethylethyl)diphenylsilyl>oxy>ethyl>-2,2-dimethyl-1,3-dioxan-4-yl>ethyl>-4-methyl-2-cyclohexen-1-one

<4R-<4α(4R*,5R*),6α>>-5-<2-<6-<2-<<(1,1-dimethylethyl)diphenylsilyl>oxy>ethyl>-2,2-dimethyl-1,3-dioxan-4-yl>ethyl>-4-methyl-2-cyclohexen-1-one

2-methyl-butyric acid 8-{2-[4-(tert-butyl-dimethyl-silanyloxy)-6-oxo-tetrahydro-pyran-2-yl]-ethyl}-7-methyl-6-oxo-1,2,6,7,8,8a-hexahydro-naphthalen-1-yl ester

2-methyl-butyric acid 8-{2-[4-(tert-butyl-dimethyl-silanyloxy)-6-oxo-tetrahydro-pyran-2-yl]-ethyl}-7-methyl-6-oxo-1,2,6,7,8,8a-hexahydro-naphthalen-1-yl ester

(S)-(1S,4S,6S,7R,8S,8aR)-4-chloro-6-(formyloxy)-8-(2-((2R,4R)-4-hydroxy-6-oxotetrahydro-2H-pyran-2-yl)ethyl)-7-methyl-1,2,3,4,6,7,8,8a-octahydronaphthalen-1-yl 2-methylbutanoate

(S)-(1S,4S,6S,7R,8S,8aR)-4-chloro-6-(formyloxy)-8-(2-((2R,4R)-4-hydroxy-6-oxotetrahydro-2H-pyran-2-yl)ethyl)-7-methyl-1,2,3,4,6,7,8,8a-octahydronaphthalen-1-yl 2-methylbutanoate

下游产品

共找到9个下游商品 >

4-(叔丁基二甲基甲硅烷氧基)-6-[2-(8-羟基-2,6-二甲基-1,2,6,7,8,8a-六氢萘)-乙基]-四氢吡喃-2-酮

4-(叔丁基二甲基甲硅烷氧基)-6-[2-(8-羟基-2,6-二甲基-1,2,6,7,8,8a-六氢萘)-乙基]-四氢吡喃-2-酮

洛伐他汀钠

洛伐他汀钠

(4R,6R)-4-hydroxy-6-(2-((1S,2S,6R,8S,8aR)-8-hydroxy-2,6-dimethyl-1,2,6,7,8,8a-hexahydronaphthalen-1-yl)ethyl)tetrahydro-2H-pyran-2-one

(4R,6R)-4-hydroxy-6-(2-((1S,2S,6R,8S,8aR)-8-hydroxy-2,6-dimethyl-1,2,6,7,8,8a-hexahydronaphthalen-1-yl)ethyl)tetrahydro-2H-pyran-2-one

alpha,beta-去氢洛伐他汀

alpha,beta-去氢洛伐他汀

莫那可林J酸

莫那可林J酸

上游原料

4-(叔丁基二甲基甲硅烷氧基)-6-[2-(8-羟基-2,6-二甲基-1,2,6,7,8,8a-六氢萘)-乙基]-四氢吡喃-2-酮 <4S-<4α,5α(4S*,6R*),6β(1R*,3S*)>>-5-<2-<6-<2-<<(1,1-dimethylethyl)diphenylsilyl>oxy>ethyl>-2,2-dimethyl-1,3-dioxan-4-yl>ethyl>-4-methyl-6-<3-methyl-1-<(triethylsilyl)oxy>-4-pentenyl>-2-cyclohexen-1-one 洛伐他汀钠 <4R-<4α(4R*,5R*),6α>>-5-<2-<6-<2-<<(1,1-dimethylethyl)diphenylsilyl>oxy>ethyl>-2,2-dimethyl-1,3-dioxan-4-yl>ethyl>-4-methyl-2-cyclohexen-1-one 2-methyl-butyric acid 8-{2-[4-(tert-butyl-dimethyl-silanyloxy)-6-oxo-tetrahydro-pyran-2-yl]-ethyl}-7-methyl-6-oxo-1,2,6,7,8,8a-hexahydro-naphthalen-1-yl ester (S)-(1S,4S,6S,7R,8S,8aR)-4-chloro-6-(formyloxy)-8-(2-((2R,4R)-4-hydroxy-6-oxotetrahydro-2H-pyran-2-yl)ethyl)-7-methyl-1,2,3,4,6,7,8,8a-octahydronaphthalen-1-yl 2-methylbutanoate (S)-(+)-2-甲基丁酸酐 (S)-2-甲基丁酰氯 (1S,3S,7R,8R,8aR)-8-(2-((2R,4R)-4-((tert-butyldimethylsilyl)oxy)-6-oxotetrahydro-2H-pyran-2-yl)ethyl)-3,7-dimethyl-6-oxo-1,2,3,4,6,7,8,8a-octahydronaphthalen-1-yl (S)-2-methylbutanoate (1S,4S,7R,8R,8aR)-8-(2-((2R,4R)-4-((tert-butyldimethylsilyl)oxy)-6-oxotetrahydro-2H-pyran-2-yl)ethyl)-4-chloro-7-methyl-6-oxo-1,2,3,4,6,7,8,8a-octahydronaphthalen-1-yl (S)-2-methylbutanoate (S)-2-Methyl-butyric acid (1S,3R,7R,8R,8aR)-8-{2-[(2R,4R)-4-(tert-butyl-dimethyl-silanyloxy)-6-oxo-tetrahydro-pyran-2-yl]-ethyl}-3,7-dimethyl-6-oxo-1,2,3,5,6,7,8,8a-octahydro-naphthalen-1-yl ester (1S-(1α,3α,7β,8β(4Σ*,6R*)8aβ))-((8-(2-(6-(2-(((1,1-dimethylethyl)diphenylsilyl)oxy)ethyl)-2,2-dimethyl-1,3-dioxan-4-yl)ethyl)-1,2,3,7,8,8a-hexahydro-3,7-dimethyl-1-naphthalenyl)oxy)triethylsilane (1S-(1α(αS,γR*),5β,6β(4Σ*,6R*)))-6-(2-(6-(2-(((1,1-dimethylethyl)diphenylsilyl)oxy)ethyl)-2,2-dimethyl-1,3-dioxan-4-yl)ethyl)-α,5-dimethyl-2-oxo-γ-((triethylsilyl)oxy)-3-cyclohexene-1-butanal (S)-2-Methyl-butyric acid (1S,3R,7R,8R,8aR)-8-{2-[(2R,4R)-4-(tert-butyl-dimethyl-silanyloxy)-6-oxo-tetrahydro-pyran-2-yl]-ethyl}-3,7-dimethyl-6-trifluoromethanesulfonyloxy-1,2,3,7,8,8a-hexahydro-naphthalen-1-yl ester (1S-(1α(R*),3α,7β,8β(4S*,6R*),8aβ))-8-(2-(6-(2-(((1,1-dimethylethyl)diphenylsilyl)oxy)ethyl)-2,2-dimethyl-1,3-dioxan-4-yl)ethyl)-1,2,3,7,8,8a-hexahydro-3,7-dimethyl-1-naphthalenyl 2-methylbutanoate (1S-(1α,3α,7β,8β(4S*,6R*),8aβ))-8-(2-(6-(2-(((1,1-dimethylethyl)diphenylsilyl)oxy)ethyl)-2,2-dimethyl-1,3-dioxan-4-yl)ethyl)-1,2,3,7,8,8a-hexahydro-3,7-dimethyl-1-naphthalenol <4S-<4α,5α(4S*,4S*),6β(1R*,3S*)>>-5-<2-<6-<2-<<(1,1-dimethylethyl)diphenylsilyl>oxy>ethyl>-2,2-dimethyl-1,3-dioxan-4-yl>ethyl>-6-(1-hydroxy-3-methyl-4-pentenyl)-4-methyl-2-cyclohexen-1-one (1S,3R,7S,8S,8aR)-8-{2-[(4R,6S)-6-(2-Hydroxy-ethyl)-2,2-dimethyl-[1,3]dioxan-4-yl]-ethyl}-3,7-dimethyl-1,2,3,7,8,8a-hexahydro-naphthalen-1-ol (1S-(1α(R*),3α,7β,8β(4S*,6R*),8aβ))-8-(2-(2,2-dimethyl-6-(2-oxoethyl)-1,3-dioxan-4-yl)ethyl)-3,7-dimethyl-1,2,3,7,8,8a-hexahydro-1-naphthalenyl 2-methylbutanoate (1S-(1α(R*),3α,7β,8β(4S*,6R*),8aβ))-1,2,3,7,8,8a-hexahydro-8-(2-(6-(2-hydroxyethyl)-2,2-dimethyl-1,3-dioxan-4-yl)ethyl)-3,7-dimethyl-1-naphthalenyl 2-methylbutanoate 6(R)-[2-[1,2,6,7,8,8a(R)-Hexahydro-2(S),6(R)-dimethyl-8(S)-[[2(S)-methylbutyryl]oxy]-1(S)-naphtyl]ethyl]-3,4,5,6-tetrahydro-4(R)-[(tert-butyldimethylsilyl)oxy]-2H-pyran-2-one

下游产品

4-(叔丁基二甲基甲硅烷氧基)-6-[2-(8-羟基-2,6-二甲基-1,2,6,7,8,8a-六氢萘)-乙基]-四氢吡喃-2-酮丙酮洛伐他汀钠 (4R,6R)-4-hydroxy-6-(2-((1S,2S,6R,8S,8aR)-8-hydroxy-2,6-dimethyl-1,2,6,7,8,8a-hexahydronaphthalen-1-yl)ethyl)tetrahydro-2H-pyran-2-one alpha,beta-去氢洛伐他汀莫那可林J酸辛伐他汀叔丁醇洛伐他汀钠