CAS: 87760-53-0; Tandospirone
该化合物是一种主要用于治疗焦虑性失调症的厌毒药物,它属于被称为zapirones的药物类别,其特征是其独特的化学结构,包括一种双环系统.该物质具有选择性的血清素受体激动剂作用,特别是针对5-HT1A受体,该受体在调和情绪和焦虑方面起着关键作用.Tandospirone以其相对作用相对较低的副作用特征而著称,它比传统的苯并二氮杂卓类相对而言是一种优先选择,因此它是长期治疗焦虑的一种选择.它通常通过口服方式进行,并具有中度作用的开端. 探虫素的药性皮肤运动表明,它具有良好的吸收性,具有能够有效治疗水平的生物可用性.此外,它具有一种有利的安全特征,其依赖性或退缩症状风险最小,是其他轴心病的重要优势.总体来说,在焦虑症的药理管理中,坦多spirone是一种宝贵的选择.
- 英文名称Tandospirone
- 中文名称坦度螺酮
- IUPAC名称(3aR,4S,7R,7aS)-2-(4-(4-(pyrimidin-2-yl)piperazin-1-yl)butyl)hexahydro-1H-4,7-methanoisoindole-1,3(2H)-dione
- 其它别名3a,4,7,7a-Hexahydro-2-(4-(4-(2-pyrimidinyl)-1-piperazinyl)butyl)-4,7-methano-1H-isoindole-1,3(2H)-dione
- CAS编号87760-53-0
- MFCD编号:MFCD00904852
- EINECS号:685-029-2
- FDA UNII编号:190230I669
- 分子式:C21H29N5O2分子量:383.49
- 产品CID: 1886222
- 同类组份化合物CAS87760-53-0 (free base)99095-10-0 (HCl)112457-95-1 (citrate)
- 产品分类原料药 → 神经系统用药 → 抗精神病药
物理性质
- 熔点112-113.5°
- 沸点613.9±65.0 °C at 760 mmHg
- 闪点325.1±34.3 °C
- 密度1.2±0.1 g/cm3
- pKa:7.71±0.10(预测)
- PSA:69.64
- LogP:2.02
- 折射率1.589
- 蒸汽压0.0±1.8 mmHg at 25°C
- 溶解性DMSO: Soluble38mg/mL
- 敏感性柠檬酸坦度螺酮(Tandospirone Citrate)：C2Lh29N5O2 C6H8O7。[112457-95-1]。盐酸坦度螺酮(Tandospimne Hydr°Chloride)：C2lH29N5O2 HCl。从异丙醇结晶，熔点227～229°C。
- 外观形态白色至类白色固体
- 储存条件储存在 +4°C
- 产品应用坦度螺酮(87760-53-0)的用途:该药是5HT1A部分激动剂.用于治疗忧郁症.
MSDS等安全信息
欧盟法规
ECHA物质C&L通报上下游产品
CAS号120596-77-2 (1R*,2S*,3R*,4S... | CAS号20980-22-7 1-(2-嘧啶基)哌嗪 | CAS号2746-19-2 顺-5-降冰片烯-外型-2,3-二甲酸酐 | CAS号14805-29-9 (3aR,4S,7R,7aS)... | CAS号14166-28-0 顺式-2,3-降冰片烷二羧酸酐 | CAS号81461-73-6 8-(2-Pyrimidiny... | CAS号33386-20-8 4-氨基丁基-1-(2-嘧啶)-哌嗪 | CAS号33386-14-0 4-(4-pyrimidin-...合成工艺路线路线简述
- 合成目标产物 Tandospirone 主要起始原料 (3Ar,4S,7R,7As) 4,7-Methano-1H-Isoindole-1,3(2H)-Dione
- 138332-79-3 = 87760-53-0
反应条件:1.1 Reagents: Hydrogen Catalysts: Palladium Solvents: Ethyl Acetate; 1.5 H,Rt
标题:Method For Preparation Of Tandospirone And Its Analogues
参考文献:China]
105981-38-2 = 87760-53-0
反应条件:1.1 Reagents: 2,6-Dimethyl-1,4-Benzoquinone Catalysts: Palladium Diacetate,4,5-Dihydro-2-[5-Methoxy-2-[(4-Methylphenyl)Sulfinyl]Phenyl]-4,4-Dimethyloxazole Solvents: Dibutyl Phosphate,1,4-Dioxane; 48 - 72 H,45 °C
标题:Allylic C-H Amination Cross-Coupling Furnishes Tertiary Amines By Electrophilic Metal Catalysis
作者:Ali,Siraj Z.; Et Al
参考文献:Science (Washington 日期:2022 卷标:376(6590) 页码:276-283]
33386-20-8 + 2746-19-2 = 87760-53-0
反应条件:1.1 Reagents: Potassium Carbonate Solvents: 1-Butanol; 7 H,120 °C2.1 Reagents: Hydrogen Catalysts: Palladium Solvents: Ethyl Acetate; 1.5 H,Rt
标题:Method For Preparation Of Tandospirone And Its Analogues
参考文献:China]
129-64-6 = 87760-53-0
反应条件:1.1 Solvents: Ethyl Acetate; 2 H,Rt -> Reflux2.1 Reagents: Potassium Carbonate Solvents: 1-Butanol; 7 H,120 °C3.1 Reagents: Hydrogen Catalysts: Palladium Solvents: Ethyl Acetate; 1.5 H,Rt
标题:Method For Preparation Of Tandospirone And Its Analogues
参考文献:China
海关参考信息
- 2912110000-甲醛
2912120000-乙醛
2921211000-乙二胺
2924191000-二甲基甲酰胺 - 💡 提示：海关信息按照顺序优先匹配，如需确认的海关信息，请参考相关资料。
- 详情请参考：📖 海关编码查询和海关进出口税则
专利信息
专利号:US-10005720-B2
优先权日:2013-04-05
标题:Compounds useful for the treatment of metabolic disorders and synthesis of the same
发明人：SEXTON JONATHAN Z; BRENMAN JAY E; MUSSO DAVID L
权利人:NORTH CAROLINA CENTRAL UNIV; UNIV NORTH CAROLINA CHAPEL HILL
摘要:The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.
专利号:US-2008214827-A1
优先权日:2004-02-03
标 题:Synthesis of Cyanoimino-Benzoimidazoles
发明人：GOEHRING R RICHARD; WHITEHEAD JOHN; SHAO BIN
权利人:EURO CELTIQUE SA
摘要:Disclosed in certain embodiments is a process for synthesizing a compound of formula (V) and salts thereof.
专利号:US-2018370905-A1
优先权日:2013-04-05
标题:Compounds Useful for the Treatment of Metabolic Disorders and Synthesis of the Same
专利号:US-9884844-B2
优先权日:2012-12-31
标 题:Heterocyclic compounds and methods of use thereof
发明人：FANG QUN KEVIN; CAMPBELL UNA; SPEAR KERRY L
权利人:SUNOVION PHARMACEUTICALS INC; SUNOVION PHARMACEUTICALS INC
摘要:Provided herein are heterocyclyl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia.
专利号:US-7749985-B2
优先权日:2006-09-15
标 题 :Acyloxyalkyl carbamate prodrugs, methods of synthesis and use
发明人：GALLOP MARK A; XU FENG; PHAN THU; DILIP USHA; PENG GE
权利人:XENOPORT INC
摘要:Acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic acid and analogs thereof, methods of making acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic acid and analogs thereof, methods of using acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic acid and analogs thereof, and pharmaceutical compositions comprising acyloxyalkyl carbamate prodrugs 3-aminopropylphosphinic acid and analogs thereof for treating diseases or disorders such as mild cognitive impairment, cognitive impairment associated with Alzheimer's disease Alzheimer's disease, depression, anxiety, and epilepsy are disclosed. Acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic acid and analogs thereof, which are suitable for oral administration and sustained release oral dosage forms are also disclosed.
专利号:CA-2555219-A1
优先权日:2004-02-03
标 题 :Synthesis of cyanoimino-benzoimidazoles
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品牌试剂参考报价(招募中)
📌 第三方产品分析报告
合成参考文献
参考文献:10.1007/s00535-005-1687-8
摘要:Hojo M, Miwa H, Yokoyama T, Ohkusa T, Nagahara A, Kawabe M, Asaoka D, Izumi Y, Sato N. Treatment of functional dyspepsia with antianxiety or antidepressive agents: systematic review. J Gastroenterol. 2005 Nov;40(11):1036–42. doi: 10.1007/s00535-005-1687-8.
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