856866-72-3

• 常用中文名：特地唑胺
• 常用英文名：Tedizolid
• CAS号：856866-72-3
• 分子式：C₁₇H₁₅FN₆O₃
• 分子量：370.338
• 相关类别： 原料药 人工合成抗感染类药 抗真菌类药
• 发布时间：2018-08-21 16:00:39
• 更新时间：2026-07-01 15:46:35
• Tedizolid是一种新型恶唑烷酮,通过与核糖体50S亚基的23S核糖体RNA结合来抑制细菌 (bacterial) 的蛋白质合成。

名称

• 中文名: 3-[3-氟-4-[6-(2-甲基-2H-四唑-5-基)-3-吡啶基]苯基]-5-(羟基甲基)-2-恶唑烷酮
• 英文名: tedizolid
• 中文别名: 特地唑胺 (MAO-A抑制剂); (R)-3-(3-氟-4-(6-(2-甲基-2H-四唑-5-基)吡啶-3-基)苯基)-5-(羟甲基)恶唑烷-2-酮,特地唑胺; 特地唑胺;特地唑胺磷酸酯; TOREZOLID 磷酸特地唑胺有关物质I杂质1.10; (R)-3-(4-(2-(2-甲基四唑-5-基)吡啶-5-基)-3-氟苯基)-5-羟甲基噁唑烷-2-酮; 替唑唑; mmu-miR-5099 mimicmmu-miR-5099 模拟物; (R)-3-(3-氟-4-(6-(2-甲基-2H-四唑-5-基)吡啶-3-基)苯基)-5-(羟甲基)噁唑烷-2-(特地唑胺杂质); 特地唑胺/泰地唑胺; 3-[3-氟-4-[6-(2-甲基-2H-四唑-5-基)-3-吡啶基]苯基]-5-(羟基甲基)-2-恶唑烷酮856-3; 特地唑胺-[13C, D3]/精确称量; 特地唑胺杂质7; 特地唑胺杂质23对照品; (R)-3-(3-氟-4-(6-(2-甲基-2H-四唑-5-基)吡啶-3-基)苯基)-5-(羟甲基)噁唑烷-2-酮(泰地唑啉杂质); 特地唑胺杂质47; (5R)-3-[3-氟-4-[6-(2-甲基-2H-四唑-5-基)-3-吡啶基]苯基]-5-(羟甲基)-2-恶唑烷酮; (R)-3-(3-氟-4-(6-(2-甲基-2H-四唑-5-基)吡啶-3-基)苯基)-5-(羟甲基)恶唑烷-2-酮; 特地唑胺杂质; 特地唑胺游离碱; 特地佐利; 特地唑胺 TEDIZOLID; 特地唑胺杂质23; (5R)-3-[3-氟-4-[6-(2-甲基-2H-四唑-5-基)-3-吡啶基]苯基]-5-(羟甲基)-2-噁唑酮; 磷酸特地唑胺TR-700; 磷酸特地唑胺M2; 泰地唑利; 特地唑啉; 抑制剂Tedizolid; 泰地唑胺杂质7; 特地唑胺BASE; 替地唑胺
• 英文别名: 3-(4-(2-(2-Methyltetrazol-5-yl)pyridine-5-yl)-3-fluorophenyl)-5-hydroxyMethyl oxazolidin-2-one; 3-[3-Fluoro-4-[6-(2-methyl-2H-tetrazol-5-yl)-3-pyridinyl]phenyl]-5-(hydroxymethyl)-2-oxazolidinone Torezolid (TR-701; (R)-3-(3-Fluoro-4-(6-(2-methyl-2H-tetrazol-5-yl)pyridin-3-yl)phenyl)-5-(hydroxymethyl)oxazolidin-2-one (Tedizolid Impurity); Torezolid856-3; Torezolid-21; (5R)-3-{3-Fluoro-4-[6-(2-methyl-2H-tetrazol-5-yl)-3-pyridinyl]phenyl}-5-(hydroxymethyl)-1,3-oxazolidin-2-one; Tedizolid (TR; Torezolid; TR-701; 3-[3-Fluoro-4-[6-(2-methyl-2H-tetrazol-5-yl)-3-pyridinyl]phenyl]-5-(hydroxymethyl)-2-oxazolidi; TR-700; DA-7157，Torezolid,TR; Tedizolid Impurity 47; 3-[3-Fluoro-4-[6-(2-methyl-2H-tetrazol-5-yl)-3-pyridinyl]phenyl]-5-(hydroxymethyl)-2-oxazolidinone; Specially thiazole amine; (R)-3-(3-fluoro-4-(6-(2-Methyl-2H-tetrazol-5-yl)pyridin-3-yl)phenyl)-5- (hydroxyMethyl)oxazolidin-2-one, Free base; (5R)-3-{3-fluoro-4-[6-(2-methyl-2H-tetrazol-5-yl)pyridin-3-yl]phenyl}-5-(hydroxymethyl)-2-oxazolidinone; (R)-3-(3-fluoro-4-(6-(2-methyl-2H-tetrazol-5-yl)pyridin-3-yl)phenyl)-5-(hydroxymethyl)oxazolidin-2-one，Torezolid; Torezolid Related substance I Impurity 1.10; (5R)-3-[3-fluoro-4-[6-(2-methyltetrazol-5-yl)pyridin-3-yl]phenyl]-5-(hydroxymethyl)-1,3-oxazolidin-2-one; (5R)-3-{3-Fluoro-4-[6-(2-Methyl-2H-Tetrazol-5-yl)-Pyridin-3-yl]-Phenyl}-5-Hydroxymethyl-Oxazolidin-2-One; (R)-3-(4-(2-(2-methyltetrazol-5-yl)pyridin-5-yl)-3-fluorophenyl)-5-hydroxymethyl oxazolidin-2-one; (R)-3-(3-fluoro-4-(6-(2-Methyl-2H-tetrazol-5-yl)pyridin-3-yl)phenyl)-5-(hydroxyMethyl)oxazolidin-2-one; (R)-3-(3-Fluoro-4-(6-(2-methyl-2H-tetrazol-5-yl)pyridin-3-yl)phenyl)-5-(hydroxymethyl)oxazolid; Torezolid (TR-701; (5R)-3-{3-fluoro-4-[6-(2-Methyl-2H-tetrazol-5-yl)pyridin-3-yl]phenyl}-5-(hydroxyMethyl)-1,3-oxazolidin-2-one Phosphate; 2-Oxazolidinone, 3-[3-fluoro-4-[6-(2-methyl-2H-tetrazol-5-yl)-3-pyridinyl]phenyl]-5-(hydroxymethyl)-, (5R); Specially acetazolaMide; Tedizolidted; (R)-3-(3-fluoro-4-(6-(2-methyl-2H; Terazolamide impurity 23; 3-(4-(2-(2-Methyltetrazol-5-yl)pyridine-5-yl)-3-fluorophenyl)-5-hydroxyMethyl oxazolidin-2-one phosphate; Tedizolid HCl(free base); Tedizolid impurity580; (5R)-3-[3-fluoro-4-[6-(2-methyl-2H-tetrazol-5-yl)-3-pyridinyl]phenyl]-5-(hydroxymethyl)-2-Oxazolidin; (R)-3-(4-(2-(2-Methyltetrazol-5-yl)pyridine-5-yl)-3-fluorophenyl)-5-hydroxyMethyl oxazolidin-2-one; Tedizolid [USAN:INN]; Torezolid //BP; DA-7157; Tedizolid (TR-701); TEDIZOLID;TR-700; DA-7157; 3-(3-fluoro-4-(6-(2-methyl-2H-tetrazol-5-yl)pyridin-3-yl)phenyl)-5-(hydroxymethyl)oxazolidin-2-one; UNII:97HLQ82NGL; 3- [3-fluoro-4- [6- (2-methyl-2H- tetrazol-5-yl) -3-pyridinyl] phenyl] -5- (hydroxymethyl) -2-oxazolidine ketone; Tedizolid free base; benzenepropanoicacid,6-chloro-β-oxo-,ethylester

物化性质

• 密度: 1.6±0.1 g/cm3
• 沸点: 614.5±65.0 °C at 760 mmHg
• 分子式: C₁₇H₁₅FN₆O₃
• 分子量: 370.338
• 闪点: 325.4±34.3 °C
• 精确质量: 370.118958
• PSA: 106.26000
• LogP: 1.56
• 外观性状: 白色至类白色固体
• 蒸汽压: 0.0±1.9 mmHg at 25°C
• 折射率: 1.725
• 储存条件: 2-8℃，干燥

生物活性

• 描述: Tedizolid是一种新型恶唑烷酮,通过与核糖体50S亚基的23S核糖体RNA结合来抑制细菌 (bacterial) 的蛋白质合成。
• 相关类别:
  信号通路 >> 抗感染 >> 细菌
  研究领域 >> 感染
• 体外研究: Tedizolid(0.25μg/ mL)抑制所有28种PRSP临床分离株,比利奈唑胺对PRSP的效力高4倍[1]。
• 体内研究: 对于用PSSP III型感染的小鼠,使用最低总日剂量10mg/kg的tedizolid磷酸盐实现100％存活率。用tedizolid磷酸盐治疗的感染小鼠的肺显示出较少的严重炎症和水肿,如炎症和水肿的平均评分所示[1]。
• 动物实验: 为了诱导全身性肺炎链球菌感染，将雄性ICR小鼠（体重18至20g）腹膜内接种悬浮于10％粘蛋白中的4种PRSP分离物（DR9，DR10，DR11或DR14）中的1种。悬浮液含有足够的细菌以杀死100％未处理的对照小鼠。在感染后1小时，小鼠接受单剂量的tedizolid磷酸盐或利奈唑胺，并且在感染后每天评估存活7天。以四种剂量（40mg / kg体重，13.33mg / kg，4.44mg / kg和1.48mg / kg）中的每一种口服和静脉内递送治疗，每组8只小鼠由剂量，递送方法定义，并感染菌株。使用概率单位分析计算每种递送途径的50％有效剂量（ED50），即允许50％感染小鼠存活的剂量。
• 参考文献:

  [1]. Choi S, et al. Activity of Tedizolid Phosphate (TR-701) in Murine Models of Infection with Penicillin-resistant and Penicillin-sensitive Streptococcus pneumoniae. Antimicrob Agents Chemother. 2012 Jun 19.

安全

• 海关编码: 29339900

合成路线

1220910-89-3 60456-26-0 ~84% 856866-72-3

文献：TRIUS THERAPEUTICS; COSTELLO, Carrie, A.; SIMSON, Jaqueline, A.; DUGUID, Robert, J.; PHILLIPSON, Douglas Patent: WO2010/42887 A2, 2010 ; Location in patent: Page/Page column 19-20 ;

624-28-2 ~% 856866-72-3

文献：European Journal of Medicinal Chemistry, , vol. 46, # 4 p. 1027 - 1039

97483-77-7 ~% 856866-72-3

文献：European Journal of Medicinal Chemistry, , vol. 46, # 4 p. 1027 - 1039

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