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CAS 220241-61-2

(3aR,4S,6R,6aS)-6-(7-chloro-5-(propylthio)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-3-yl)-2,2-dimethyltetrahydro-4H-cyclopenta[d][1,3]dioxol-4-ol

Codes：TICA-005

Application context (from source-drug indications)

中风替格瑞洛急性冠脉综合征替格瑞洛心肌梗塞替格瑞洛外周血管疾病替格瑞洛

Source drugs (routes using this intermediate)

DrugTierExpiry
替格瑞洛TicagrelorTier B — Position early2029

Position in synthesis routes (up/downstream chain)

Ordered by route registration; left → right is the synthesis direction. The highlighted node is the current CAS; others link to their own profiles.

替格瑞洛原研路线steps: 9total yield: /
4,6-dichloro-5-nitro-2-(propylthio)pyrimidine→(3aR,4S,6R,6aS)-6-amino-2,2-dimethyltetrahydro-4H-cyclopenta[d][1,3]dioxol-4-ol→(3aR,4S,6R,6aS)-6-((6-chloro-5-nitro-2-(propylthio)pyrimidin-4-yl)amino)-2,2-dimethyltetrahydro-4H-cyclopenta[d][1,3]dioxol-4-ol→(3aR,4S,6R,6aS)-6-((5-amino-6-chloro-2-(propylthio)pyrimidin-4-yl)amino)-2,2-dimethyltetrahydro-4H-cyclopenta[d][1,3]dioxol-4-ol→(3aR,4S,6R,6aS)-6-(7-chloro-5-(propylthio)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-3-yl)-2,2-dimethyltetrahydro-4H-cyclopenta[d][1,3]dioxol-4-ol→(3aR,4S,6R,6aS)-6-(7-amino-5-(propylthio)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-3-yl)-2,2-dimethyltetrahydro-4H-cyclopenta[d][1,3]dioxol-4-ol→methyl 2-(((trifluoromethyl)sulfonyl)oxy)acetate→methyl 2-(((3aR,4S,6R,6aS)-6-(7-amino-5-(propylthio)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-3-yl)-2,2-dimethyltetrahydro-4H-cyclopenta[d][1,3]dioxol-4-yl)oxy)acetate→methyl 2-(((3aR,4S,6R,6aS)-6-(7-bromo-5-(propylthio)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-3-yl)-2,2-dimethyltetrahydro-4H-cyclopenta[d][1,3]dioxol-4-yl)oxy)acetate→(1R,2S)-2-(3,4-difluorophenyl)cyclopropan-1-amine→methyl 2-(((3aR,4S,6R,6aS)-6-(7-(((1R,2S)-2-(3,4-difluorophenyl)cyclopropyl)amino)-5-(propylthio)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-3-yl)-2,2-dimethyltetrahydro-4H-cyclopenta[d][1,3]dioxol-4-yl)oxy)acetate→potassium sodium (2R,3R)-2,3-dihydroxysuccinate→2-(((3aR,4S,6R,6aS)-6-(7-(((1R,2S)-2-(3,4-difluorophenyl)cyclopropyl)amino)-5-(propylthio)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-3-yl)-2,2-dimethyltetrahydro-4H-cyclopenta[d][1,3]dioxol-4-yl)oxy)ethan-1-ol→(1R,4S)-4-hydroxycyclopent-2-en-1-yl acetate→TICA-015→TICA-016→4-methylmorpholine 4-oxide→TICA-018→2,2-dimethoxypropane

Intermediates available on this site

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SupplierProductPrice bandMOQLead timeQualifications
Qualified Partner — East China API Works4,6-Dichloro-2-(propylthio)pyrimidin -5-amine
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Unibest Nantong cGMP Site2-((3aR,4S,6R,6aS)-6-amino-2,2-dimethyltetrahydro -3aH-cyclopenta[d][1,3]dioxol -4-yloxy)ethanol L-tataric acid
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Unibest Taizhou GMP-like Site(1R,2S)-2-(3,4-Difluorophenyl)cyclopropanaminium(2R)hydroxy(phenyl)ethanoate
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Qualified Partner — East China API WorksEthanol, 2-[[(3aR,4S,6R,6aS)-6-[[5-aMino-6-chloro-2-(propylthio)-4-pyriMidinyl]aMino]tetrahydro-2,2-diMethyl-4H-cyclopenta-1,3-dioxol-4-yl]oxy]-
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Unibest Nantong cGMP Site(1R,2S)-2-(3,4-difluorophenyl)cyclopropanamine hydrochloride
Pharmaceutical Intermediates
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Unibest Taizhou GMP-like SiteCyclopropanamine,2-(3,4-difluorophenyl)-(1R,2S) -(2R,3R)-2,3-dihydroxybutanedioate (1:1)
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Qualified Partner — East China API Works2-[[(3aS,4R,6S,6aR)-4-[7-[[(1R,2S)-2-(3,4-Difluorophenyl)cyclopropyl]amino]-5-(propylthio)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-3-yl]-2,2-dimethyl-tetrahydro-3aH-cyclopenta[d][1,3]dioxol-6-yl]oxy]ethanol
Pharmaceutical Intermediates
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