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富马酸喹硫平

富马酸喹硫平用途

【用途一】
抗精神病药.

富马酸喹硫平名称

[ CAS 号 ]:
111974-72-2

[ 中文名 ]:
喹硫平半富马酸盐

[ 英文名 ]:
Quetiapine Fumarate

[中文别名 ]:

[英文别名 ]:

MFCD03423782
Quetiapine Hemifumarate
Quetiapine fumarate
Quetiapine hemifumarate salt
Quetiapine (fumarate)

富马酸喹硫平生物活性

[ 描述 ]:

Quetiapine富马酸盐是非典型的抗精神病化合物,可作用于精神分裂,两极忧郁症等。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 5-HT受体

信号通路 >> 神经信号通路 >> 5-HT受体

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 多巴胺受体

信号通路 >> 神经信号通路 >> 多巴胺受体

研究领域 >> 神经疾病

[参考文献]

[1]. Sheehan DV, Locklear J, Sveds?ter H, Datto C. Long-term functioning and sleep quality in patients with major depressive disorder treated with extended-release quetiapine fumarate. Int Clin Psychopharmacol. 2012 Sep;27(5):239-48.

[2]. Endicott J, Sveds?ter H, Locklear JC. Effects of once-daily extended release quetiapine fumarate on patient-reported outcomes in patients with generalized anxiety disorder. Neuropsychiatr Dis Treat. 2012;8:301-311.

[3]. Lee JG, Lee JI, Kim YT, Kim CE, Kim CY, Yoon JS, Yoo SY, Kim YH. Safety of quetiapine fumarate extended release in the treatment of Korean patients with acute schizophrenia. Hum Psychopharmacol. 2012 Jul;27(4):403-10. doi: 10.1002/hup.2241.

[4]. Thase ME, Demyttenaere K, Earley WR, Gustafsson U, Udd M, Eriksson H. Extended release quetiapine fumarate in major depressive disorder: analysis in patients with anxious depression. Depress Anxiety. 2012 Jul;29(7):574-86. doi: 10.1002/da.21970.

[5]. Katila H, Mezhebovsky I, Mulroy A, Berggren L, Eriksson H, Earley W, Datto C. Randomized, Double-Blind Study of the Efficacy and Tolerability of Extended Release Quetiapine Fumarate (Quetiapine XR) Monotherapy in Elderly Patients With Major Depressive Di

[相关活性小分子]

富马酸喹硫平物理化学性质

[ 沸点 ]:
556.5ºC at 760 mmHg

[ 熔点 ]:
174-176°C

[ 分子式 ]:
C₂₃H₂₇N₃O₄S

[ 分子量 ]:
441.54

[ 闪点 ]:
290.4ºC

[ PSA ]:
221.80000

[ LogP ]:
4.04660

[ 外观性状 ]:
白色结晶固体

[ 蒸汽压 ]:
3.22E-13mmHg at 25°C

[ 储存条件 ]:
-20°C Freezer

[ 水溶解性 ]:
水溶性：实际上不溶；可溶于：二甲基甲酰胺；微溶：甲醇；极微溶：乙醇；不溶：乙醚

富马酸喹硫平MSDS

详细MSDS(安全技术说明书)

富马酸喹硫平安全信息

[ 符号 ]:

GHS07, GHS09

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302-H400

[ 警示性声明 ]:
P273

[ 危害码 (欧洲) ]:
T,F

[ 风险声明 (欧洲) ]:
R45:May cause cancer. R10:Flammable.

[ 安全声明 (欧洲) ]:
S53-S45

[ 危险品运输编码 ]:
UN 3295 3/PG 3

[ WGK德国 ]:
3

[ RTECS号 ]:
PC1075000

[ 包装等级 ]:
III

[ 危险类别 ]:
3

[ 海关编码 ]:
2934999090

富马酸喹硫平制备

1. 2-异氰酸基二苯硫醚的制备

在反应瓶中加入2-氨基二苯硫醚20g(0.1mol)和甲苯125ml,在0~5ºC缓慢滴加三光气11.9g(0.04mol)的甲苯50ml溶液,加毕,升温至60ºC搅拌反应1h.反应液至澄清后,通入氮气除尽产生的光气,蒸除溶剂,得无色油状物2-异氰酸基二苯硫醚22g,直接用于下步反应.

2. 10H-二苯并[b,f][1,4]硫氮杂-11-酮的制备

在反应瓶中加入上步一批量的2-异氰酸基二苯硫醚和多聚磷酸120g,升温至50ºC搅拌溶解,然后加热至100ºC搅拌反应3h.反应液由无色透明逐渐变黄,当颜色不再变化时结束反应,自然冷却至50ºC,剧烈搅拌下转

至冰水200ml中,析出固体,过滤,滤饼水洗,丙酮洗,得白色固体10H-二苯并[b,f][1,4]硫氮杂-11-酮21g, 收率96%(以2-氨基二苯醚计),mp259~260 ºC.

3. 11-氯-二苯并[b,f][1,4]硫氮杂的的制备

在反应瓶中加入POCl2 100ml(1.07mol)、N,N-二甲基苯胺6g和10H-二苯并[b,f][1,4]硫氮杂-11-酮 18.2g(0.08mol),搅拌均匀,在氮气保护下加热回流反应4h.TLC跟踪[展开剂:乙醚/石油醚(1:1),R1=0.7].反应毕,减压蒸除溶剂,剩余物为褐色糊状物,溶于甲苯250ml,搅拌下转至冰水50ml中,静置30min后,分出甲苯层,水(50m×2)洗,无水硫酸镁干燥,过滤,滤液浓缩至体积50ml,直接用于下一步反应.

4. 11-哌嗪基二苯并[b,f][1,4] 硫氮杂的制备

在反应瓶中加入上步所得的11-氯-二苯并[b,f][1,4]硫氮杂的甲苯溶液(一批量),在室温下滴加(搅拌下)无水哌嗪17.2g(0.2mol)的甲苯溶液100ml,1h内加完,加热搅拌回流3h{TLC跟踪[展开剂:乙醚/石油醚(1:1),R1=0.5]}.反应毕,过滤,滤液水(100ml×2)洗,无水硫酸镁干燥,过滤,滤液直接用于下步反应.

5. 11-[4-[2-(2-羟基乙氧基)乙基]-1-哌嗪基]二苯并[b,f][1,4]硫氮杂半富马酸盐(半富马酸喹硫平)的合成

在反应瓶中加入上步11-哌嗪基二苯并[b,f][1,4] 硫氮杂的甲苯溶液,N-甲基吡咯烷酮50ml、2-(2-氯乙氧基)乙醇10.0g(0.08mol)、Na2CO3 17.0g(0.16mol)和少量NaI,搅拌加热回流24h.TLC跟踪[展开剂:甲醇/二氯甲烷(1:9),Rf=0.5].反应毕,减压蒸除甲苯,剩余物加入乙酸乙酯200ml,冰水洗至中性,无水硫酸镁干燥,过滤,滤液减压蒸除乙酸乙酯,得油状喹硫平.将油状喹硫平溶于无水乙醇100ml,加入富马酸4.6g(0.04mol),加热搅拌回流30min,冷却,静置过夜析晶.过滤,滤饼用无水乙醇洗,干燥,得黄色晶体11-[4-[2-(2-羟基乙氧基)乙基]-1-哌嗪基]二苯并[b,f][1,4]硫氮杂半富马酸盐(半富马酸喹硫平)23.4g,收率66.3%,mp170~171.5 ºC,纯度>99%,(RP-HPLC法).

富马酸喹硫平海关

[ 海关编码 ]: 2934999090

[ 中文概述 ]:
2934999090. 其他杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

富马酸喹硫平文献

The dopaminergic stabilizers pridopidine and ordopidine enhance cortico-striatal Arc gene expression.

J. Neural Transm. Gen. Sect. 121(11) , 1337-47, (2014)

The dopaminergic stabilizers pridopidine [4-(3-(methylsulfonyl)phenyl)-1-propylpiperidine] and ordopidine [1-ethyl-4-(2-fluoro-3-(methylsulfonyl)phenyl)piperidine] inhibit psychostimulant-induced hype...

An understanding of modified release matrix tablets behavior during drug dissolution as the key for prediction of pharmaceutical product performance - case study of multimodal characterization of quetiapine fumarate tablets.

Int. J. Pharm. 484(1-2) , 235-45, (2015)

Motivation for the study was the lack of dedicated and effective research and development (R&D) in vitro methods for oral, generic, modified release formulations. The purpose of the research was to as...

Quetiapine for the treatment of cocaine use disorder.

Drug Alcohol Depend. 149 , 18-24, (2015)

Cocaine addiction continues to be a significant healthcare issue, yet there are no FDA approved medications for the treatment of cocaine use disorder within the United States.This 12-week, prospective...

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