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替格瑞洛

替格瑞洛

CAS号：274693-27-5

英文名：ticagrelor

分子式

C23H28F2N6O4S

熔点

密度

1.67

分子量

522.568

沸点

777.551ºC at 760 mmHg

溶解度

信号词

危险品标志

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化合物简介

替格瑞洛的商品名为倍林达，圆形、双凸、黄色包衣片，一面刻有“T”，其上方刻有“90”字样，另一面光滑，含90 mg的替格瑞洛。替格瑞洛是一种血小板聚集抑制剂，其临床疗效和安全性已得到血小板抑制和患者后果结局研究（PLATO研究）及其多项亚组研究2-11的验证和支持。PLATO研究也显示替格瑞洛的疗效明显优于氯吡格雷，所以被国内外多个指南列于一线推荐，且欧洲指南更是在近两年将替格瑞洛的推荐级别列于氯吡格雷之前，在替格瑞洛不能使用的患者中才能使用氯吡格雷。由于替格瑞洛与噻吩并吡啶类药物（氯吡格雷）是一种不同化学分类的药物，因此将之前的中文用名“替卡格雷”更换为“替格瑞洛”。

基本信息

中文名称

替格瑞洛

英文名称

ticagrelor

中文别名

(1S,2S,3R,5S)-3-[7-[[(1R,2S)-2-(3,4-二氟苯基)环丙基]氨基]-5-丙硫基三唑并[4,5-d]嘧啶-3-基]-5-(2-羟乙氧基)-1,2-环戊二醇、替卡格雷

英文别名

(1S,2S,3R,5S)-3-(7-(((1R,2S)-2-(3,4-difluorophenyl)cyclopropyl)amino)-5-(propylthio)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-3-yl)-5-(2-hydroxyethoxy)cyclopentane-1,2-diol、Brilique、(1S,2S,3R,5S)-3-[7-[[(1R,2S)-2-(3,4-difluorophenyl)cyclopropyl]amino]-5-propylsulfanyltriazolo[4,5-d]pyrimidin-3-yl]-5-(2-hydroxyethoxy)cyclopentane-1,2-diol、AZD 6140、TICARGRELOR、Ticagrelor、Brilinta

CAS号

274693-27-5

分子式

C23H28F2N6O4S

分子量

522.568

精确质量

522.186

PSA

163.74

LOGP

2.0867

编号系统

MDL号

MFCD09954148

物化性质

密度

1.67

沸点

777.551ºC at 760 mmHg

闪点

424.048ºC

折射率

1.744

安全信息

海关编码

2933990090

生产方法及用途

用途

原料药，用于减少急性冠脉综合征（ACS）患者的心血管死亡和心脏病发作。

合成路线

BATAMA

替格瑞洛

上游原料

共找到112个上游原料 >

N-[(3aS,4R,6S,6aR)-四氢-6-羟基-2,2-二甲基-4H-环戊烯并-1,3-二氧戊环-4-基]氨基甲酸苄酯

N-[(3aS,4R,6S,6aR)-四氢-6-羟基-2,2-二甲基-4H-环戊烯并-1,3-二氧戊环-4-基]氨基甲酸苄酯

1,2-Cyclopentanediol, 3-amino-5-(2-hydroxyethoxy)-, (1S,2S,3R,5S)-

1,2-Cyclopentanediol, 3-amino-5-(2-hydroxyethoxy)-, (1S,2S,3R,5S)-

benzyl (3aR,4S,6R,6aS)-4-(2-hydroxyethoxy)tetrahydro-3aH-spiro[cyclopenta[d][1,3]dioxole-2,1'-cyclopentane]-6-ylcarbamate

benzyl (3aR,4S,6R,6aS)-4-(2-hydroxyethoxy)tetrahydro-3aH-spiro[cyclopenta[d][1,3]dioxole-2,1'-cyclopentane]-6-ylcarbamate

ethyl 2-((3aS,4R,6S,6aR)-4-(benzyloxycarbonylamino)-tetrahydro-3aH-spiro[cyclopenta[d][1,3]dioxole-2,1'-cyclopentane]-6-yloxy)acetate

ethyl 2-((3aS,4R,6S,6aR)-4-(benzyloxycarbonylamino)-tetrahydro-3aH-spiro[cyclopenta[d][1,3]dioxole-2,1'-cyclopentane]-6-yloxy)acetate

BATAMA

(1S,2S,3R,5S)-3-(7-(benzyl((1R,2S)-2-(3,4-difluorophenyl)cyclopropyl)amino)-5-(propylthio)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-3-yl)-5-(2-hydroxyethoxy)cyclopentane-1,2-diol

(1S,2S,3R,5S)-3-(7-(benzyl((1R,2S)-2-(3,4-difluorophenyl)cyclopropyl)amino)-5-(propylthio)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-3-yl)-5-(2-hydroxyethoxy)cyclopentane-1,2-diol

上游原料

N-[(3aS,4R,6S,6aR)-四氢-6-羟基-2,2-二甲基-4H-环戊烯并-1,3-二氧戊环-4-基]氨基甲酸苄酯 1,2-Cyclopentanediol, 3-amino-5-(2-hydroxyethoxy)-, (1S,2S,3R,5S)- benzyl (3aR,4S,6R,6aS)-4-(2-hydroxyethoxy)tetrahydro-3aH-spiro[cyclopenta[d][1,3]dioxole-2,1'-cyclopentane]-6-ylcarbamate ethyl 2-((3aS,4R,6S,6aR)-4-(benzyloxycarbonylamino)-tetrahydro-3aH-spiro[cyclopenta[d][1,3]dioxole-2,1'-cyclopentane]-6-yloxy)acetate BATAMA (1S,2S,3R,5S)-3-(7-(benzyl((1R,2S)-2-(3,4-difluorophenyl)cyclopropyl)amino)-5-(propylthio)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-3-yl)-5-(2-hydroxyethoxy)cyclopentane-1,2-diol 3-chloro-1-(3',4'-difluorophenyl)-propan-1-one 2-[[(3aR,4S,6R,6aS)-6-氨基四氢-2,2-二甲基-4H-环戊烯并-1,3-二氧杂环戊烷-4-基]氧基]乙醇 4,6-二氯-2-丙基硫代嘧啶-5-胺 1-(3',4'-difluorophenyl)-3-nitro-propan-1-one (1R,2S)-2-(3,4-二氟苯基)环丙胺 (R)-扁桃酸盐 (4R,5R)-2,2-dimethyl-5-vinyl-[1,3]dioxolane-4-carbaldehyde (1R,2S)-2-(3,4-difluorophenyl)cyclopropan-1-amine mandelate N-(((4S,5R)-2,2-dimethyl-5-vinyl-1 ,3-dioxolan-4-yl)methylene)-1-phenylmethanamine oxide tert-butyl [[(3aR,4S,6R,6aS)-6-(N,N-dibenzylamino)-2,2-dimethyltetrahydro-3aH-cyclopenta[d][1,3]dioxol-4-yl]oxy]acetate benzyl (1R,2S,3S,4S)-2,3-dihydroxy-4-(2-hydroxyethoxy)-cyclopentylcarbamate (1R,2S)-2-(3,4-二氟苯基)环丙胺盐酸盐 tert-butyl (6-chloro-5-nitro-2-(propylthio)pyrimidin-4-yl)((1R,2S)-2-(3,4-difluorophenyl)cyclopropyl)carbamate trans-(1R,2S)-2-(3,4-difluorophenyl)-1-nitrocyclopropane (3aR,4S,6R,6aS)-6-[7-氯-5-(丙硫基)-3H-1,2,3-三氮唑并[4,5-d]嘧啶-3-基]四氢-2,2-二甲基-4H-环戊烯并-1,3-二恶茂-4-醇 (1S,2S,3R,5S)-3-(7-hydroxy-5-(propylthio)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-3-yl)-5-(2-hydroxyethoxy)cyclopentane-1,2-diol tetrahydro-2,2-dimethyl-6-phenylmethyl-(3aS,4S,7R,7aS)-4,7-methano-4H-1,3-dioxolo[4,5-d][1,2]oxazine tert-butyl ((3aS,4R,6S,6aR)-6-hydroxy-2,2-dimethyltetrahydro-3aH-cyclopenta[d]-[1,3]dioxol-4-yl)carbamate (3aR,4S,6R,6aS)-6-(benzylamino)-2,2-dimethyltetrahydro-3ah-cyclopenta-[d][1,3]-dioxol-4-ol N-[(3aS,4R,6S,6aR)-四氢-6-(2-羟基乙氧基)-2,2-二甲基-4H-环戊烯并-1,3-二氧杂环戊烷-4-基]氨基甲酸苯甲酯甲基-2,3-O-异亚丙基-beta-D-呋喃核糖苷 BATAMAT 6-羟基-2-(丙基硫代)-4(3h)-嘧啶酮 benzyl (3aR,4S,6R,6aS)-4-hydroxytetrahydro-3aH-spiro[cyclopenta[d][1,3]dioxole-2,1'-cyclopentane]-6-ylcarbamate 4,6-二氯-5-硝基-2-丙硫基嘧啶 2-({(3aR,4S,6R,6aS)-6-[7-{[[N-(IR,2S)-2-(3,4-difluorophenyl)-cyclopropan-1-yl]-N-benzyl]amino}-5-(propylthio)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-3-yl]-2,2-dimethyl-tetrahydro-3aH-cyclopenta[d][1,3]dioxol-4-yl}oxy)ethanol 2-({(3aR,45,6R,6aS)-6-[7-{[[N-(1R,2S)-2-(3,4-difluorophenyl)-cyclopropan-1-yl]-N-tert-butoxycarbonyl]amino}-5-(propylthio)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-3-yl]-2,2-dimethyl-tetrahydro-3aH-cyclopenta[d][1,3]dioxol-4-yl}oxy)-O-tertbutoxycarbonylethanol (3aR,4S,6R,6aS)-6-氨基四氢-2,2-二甲基-4H-环戊烯并-1,3-二氧杂环戊烷-4-醇 3,4-二氟肉桂酸 2-[[(3aR,4S,6R,6aS)-6-[[4-[N-[(1R,2S)-2-(3,4-difluorophenyl)cyclopropan-1-yl]-N-tert-butoxycarbonyl]amino] -2-(propylthio)-5-aminopyrimidin-6-yl]-2,2-dimethyl-tetrahydro-3aH-cyclopenta[d][1,3]dioxol-4-yl]oxy]ethanol (3aS,4S,6aR)-4-(iodomethyl)-6-methoxy-2,2-dimethyltetrahydrofuro[3,4-d][1,3]dioxole (2E)-3-(3,4-Difluorophenyl)acryloyl chloride (3aR,4S,6R,6aS)-6-(N,N-dibenzylamino)-2,2-dimethyltetrahydro-3aH-cyclopenta[d][1,3]dioxol-4-ol 异亚丙基替卡格雷 2-[[(3aR,4S,6R,6aS)-6-(N,N-dibenzylamino)-2,2-dimethyltetrahydro-3aH-cyclopenta[d][1,3]dioxol-4-yl]oxy]ethanol 1,2-二氟苯 (1S)-1-(3,4-difluorophenyl)-3-nitropropan-1-ol 2-[[(3aR,4S,6R,6aS)-6-[[4-[N-[(1R,2S)-2-(3,4-difluorophenyl)cyclopropan-1-yl]-N-tert-butoxycarbonyl]amino]-2-(propylthio)-5-nitropyrimidin-6-yl]-2,2-dimethyl-tetrahydro-3aH-cyclopenta[d][1,3]dioxol-4-yl]oxy] ethanol 1-甲氧基-2,3-O-异亚丙基-5-O-对甲苯磺酰基-beta-D-呋喃核糖苷