147127-20-6 泰诺福韦

泰诺福韦

英文名称:tenofovir (anhydrous)
CAS:

147127-20-6

分子式:C9H14N5O4P
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  • 物化性质
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  • 合成路线
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泰诺福韦简介

Microbicides for sexually transmitted diseases are pharmacologic agents and chemical substances that are capable of killing or destroying certain microorganisms that commonly cause human infection (for example, the human immunodeficiency virus).
Microbicides are a diverse group of chemical compounds that exert their activity by a variety of different mechanisms of action. Multiple compounds are being developed and tested for their microbicidal activity in clinical trials. Microbicides can be formulated in various delivery systems including gels, creams, lotions, aerosol sprays, tablets or films (which must be used near the time of sexual intercourse) and sponges and vaginal rings (or other devices that release the active ingredient(s) over a longer period). Some of these agents are being developed for vaginal application, and for rectal use by those engaging in anal sex.
Although there are many approaches to preventing sexually transmitted diseases in general (and HIV in particular), current methods have not been sufficient to halt the spread of these diseases (particularly among women and people in less-developed nations). Sexual abstinence is not a realistic option for women who want to bear children, or who are at risk of sexual violence. In such situations, the use of microbicides could offer both primary protection (in the absence of condoms) and secondary protection (if a condom breaks or slips off during intercourse). It is hoped that microbicides may be safe and effective in reducing the risk of HIV transmission during sexual activity with an infected partner.[full citation needed]

泰诺福韦基本信息

中文名称 泰诺福韦 英文名称 tenofovir (anhydrous)
中文别名

泰诺福韦(PMPA); (R)-9-(2-磷酸甲氧基丙基)-腺嘌呤; 替诺福韦;

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英文别名

(R)-(((1-(6-Amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)phosphonic acid; Tenofovir; (R)-(1-(6-amino-9H-purin-9-yl)propan-2-yloxy)methylphosphonic acid; D,L-TENOFOVIR; Apropovir; 9-Pmpa; Tenefovir; GS-1278;

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CAS号 147127-20-6 分子式 C9H14N5O4P
分子量 287.21200 精确质量 287.07800
PSA 146.19000 LOGP 0.53000

泰诺福韦编号系统

MDL号 MFCD00943794

泰诺福韦物化性质

外观与性状:
白色结晶固体
密度:
1.79 g/cm3
沸点:
616.1ºC at 760 mmHg
熔点:
276-280°C
闪点:
326.4ºC
水溶解性:
13.4 mg/mL (25 ºC)

安全信息

RTECS号:
DB8930000
安全说明:
S22; S26; S27; S36/37/39
危险类别码:
R34
WGK Germany:
3
海关编码:
2933990090
危险品运输编码:
UN 3261 8/PG 2
危险类别:
8
包装等级:
III
危险品标志:
C

生产方法及用途

生产方法

1.将亚磷酸二乙酯、多聚甲醛和三乙胺溶于甲苯,在氮气保护下反应,回流。反应完全后冷却,缓慢加入对甲苯磺酰氯和三乙胺,反应得到对甲苯磺酰氧甲基膦酸二乙酯。在氮气保护下,将(犛)-缩水甘油、5%钯碳、乙醇和氢氧化钠水溶液混合,进行加氢,得到(犚)-1,2-丙二醇。加入碳酸二乙酯和乙醇钠的乙醇溶液,反应得(犚)-1,2-丙二醇碳酸酯。将其和腺嘌呤、对甲苯磺酰氧甲基膦酸二乙酯、氢氧化钠溶于二甲基甲酰胺,反应得(犚)-9-[2-(二乙基膦酰基甲氧基)丙基]腺嘌呤。将其溶于乙腈,加溴三甲基硅烷,得泰诺福韦粗品,重结晶得纯品。将泰诺福韦和1-甲基-2-吡咯烷酮、三乙胺混合加入碳酸氯甲基丙基酯反应,再用富马酸酸化,得富马酸泰诺福韦双特戊酰氧基甲酯。

用途

核苷酸类似物逆转录酶抑制剂,可阻断HIV复制。与其他抗逆转录病毒药物联合应用治疗HIV-1感染。用于艾滋病的治疗。

SDS 1.0 中文 展开
SDS 1.0 英文 展开
1H NMR : Predict展开

核磁图谱 1H NMR : Predict

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国家名称 海关编码 海关数据更新时间 操作
中国 2933990090 2019-03 申报要素
美国 2933999700 2019-03 概述
印度 29339900 2019-03 概述
欧盟 29339980 2019-03 概述
英国 2933998090 2019-03 概述
日本 293399090 2019-03 概述
韩国 2933999000 2019-03 概述
加拿大 2933990090 2019-03 概述
泰诺福韦
CAS号:147127-20-6 分子式:C9H14N5O4P 分子量:287.21200

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