化合物简介
Raloxifene (marketed as Evista by Eli Lilly and Company) is an oral selective estrogen receptor modulator (SERM) that has estrogenic actions on bone and anti-estrogenic actions on the uterus and breast. It is used in the prevention of osteoporosis in postmenopausal women and to reduce the risk of invasive breast cancer in postmenopausal women with osteoporosis and in postmenopausal women at high risk for invasive breast cancer.
基本信息
中文名称
雷洛昔芬
英文名称
raloxifene
中文别名
雷洛西芬、[6-羟基-2-(4-羟苯基)苯并[b]噻酚-3-基]-[4-[2-(1-哌啶基)乙氧基]-苯基]-甲酮
英文别名
[3H]-Raloxifene、Raloxifenum、6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-piperidino-ethoxy)benzoyl]benzo[b]thiophene、[2-(4-Hydroxyphenyl)-6-hydroxybenzo[b]thien-3-yl] [4-[2-(1-piperidinyl)ethoxy]phenyl]methanone、[14C]-Raloxifene、Raloxifeno、Raloxifene [INN:BAN]、Raloxifenum [Latin]、Raloxifeno [Spanish]、Keoxifene、UNII-YX9162EO3I、[6-hydroxy-2-(4-hydroxyphenyl)-1-benzothiophen-3-yl]-[4-(2-piperidin-1-ylethoxy)phenyl]methanone
CAS号
84449-90-1
分子式
C28H27NO4S
分子量
473.583
精确质量
473.166
PSA
98.24
LOGP
6.0131
编号系统
MDL号
MFCD00866415
物化性质
外观与性状
淡黄色固体
密度
1.289 g/cm3
沸点
728.2ºC at 760 mmHg
熔点
250-253°C
闪点
394.2ºC
储存条件
Store in original container in a cool dark place.
安全信息
WGK Germany
3
生产方法及用途
生产方法
2-(4-羟基苯基)苯并[b]噻吩-6-醇经甲磺酰氯酯化，生成的二酯化物与4-(2-哌啶基乙氧基)苯甲酰氯进行酰化反应，经水解得到雷洛昔芬。
用途
雌激素受体调节剂，在子宫和乳腺组织呈现拮抗雌激素作用，抑制乳腺上皮和子宫内膜增生。在骨脂代谢方面呈现兴奋作用，具有拟雌激素作用。雷洛昔芬与钙制剂合用能预防骨的丢失，保持骨密度并有降血脂作用。
上游原料
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