替格瑞洛(Ticagrelor)杂质

1

替格瑞洛杂质A

NA

(1R,2R,3S,5R)-3-(7-(((1S,2R)-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

2

替格瑞洛杂质B

NA

(1R,2R,3S,5R)-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

3

替格瑞洛杂质C

NA

(1S,2S,3R,5S)-3-(7-(((1S,2R)-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

替格瑞洛杂质D

NA

2-(((3aR,4S,6R,6aS)-6-((3-((1R,2S)-2-(3,4-difluorophenyl)cyclopropyl)-5-(propylthio)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-7-yl)amino)-2,2-dimethyltetrahydro-3aH-cyclopenta[d][1,3]dioxol-4-yl)oxy)ethanol

4

替格瑞洛杂质E

NA

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

5

替格瑞洛杂质F

NA

2-(((1S,2S,3S,4R)-4-(7-(((1R,2S)-2-(3,4-difluorophenyl)cyclopropyl)amino)-5-(propylthio)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-3-yl)-2,3-dihydroxycyclopentyl)oxy)ethyl acetate

6

替格瑞洛杂质G

NA

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

7

替卡格雷杂质 H

NA

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

8

替卡格雷杂质 I

NA

(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

9

替卡格雷杂质 J

NA

(1S,2S,3R,5S)-3-((5-amino-6-chloro-2-(propylthio)pyrimidin-4-yl)amino)-5-(2-hydroxyethoxy)cyclopentane-1,2-diol

10

替卡格雷杂质 K

NA

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

11

替卡格雷杂质 L（亚砜）

NA

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

12

替卡格雷杂质M(砜)

NA

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

13

替卡格雷杂质 N

NA

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

14

替卡格雷杂质 O

NA

(1S,2S,3S,5S)-3-((6-chloro-5-((3-((1S,2S,3S,4S)-2,3-dihydroxy-4-(2-hydroxyethoxy)cyclopentyl)-5-(propylthio)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-7-yl)amino)-2-(propylthio)pyrimidin-4-yl)amino)-5-(2-hydroxyethoxy)cyclopentane-1,2-diol

15

替卡格雷杂质 P

NA

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

16

替卡格雷杂质 Q

NA

(1R,2R,3S,5R)-3-(4-(((1R)-2-(3,4-difluorophenyl)cyclopropyl)amino)-6-(propylthio)-1H-[1,2,3]triazolo[4,5-d]pyrimidin-1-yl)-5-(2-hydroxyethoxy)cyclopentane-1,2-diol compound with (1R,2R,3S,5R)-3-(4-(((1S,2S)-2-(3,4-difluorophenyl)cyclopropyl)amino)-6-(propylthio)-1H-[1,2,3]triazolo[4,5-d]pyrimidin-1-yl)-5-(2-hydroxyethoxy)cyclopentane-1,2-diol (1:1)

17

替卡格雷杂质 R

NA

D-酒石酸盐； 
cis-2-(3,4-difluorophenyl) cyclopropanamine
2-(((3aS,4R,6S,6aR)-6-amino-2,2-dimethyltetrahydro-3aH-cyclopenta[d][1,3]dioxol-4-yl)oxy)ethanol

18

替卡格雷杂质 S

NA

benzyl ((3aR,4S,6R,6aS)-6-(2-hydroxyethoxy)-2,2-dimethyltetrahydro-3aH-cyclopenta[d][1,3]dioxol-4-yl)carbamate

19

替卡格雷杂质 T

NA

(1S,2R)-2-(3,4-difluorophenyl)cyclopropanamine hydrochloride

20

替卡格雷杂质 U

NA

tert-butyl ((1S,2R)-2-(3,4-difluorophenyl)cyclopropyl)carbamate compound with benzyl ((3aR,4S,6R,6aS)-6-(2-hydroxyethoxy)-2,2-dimethyltetrahydro-3aH-cyclopenta[d][1,3]dioxol-4-yl)carbamate (1:1)

21

替卡格雷杂质 V

NA

2-(((3aR,4S,6R,6aS)-6-((6-chloro-5-nitro-2-(propylthio)pyrimidin-4-yl)amino)-2,2-dimethyltetrahydro-3aH-cyclopenta[d][1,3]dioxol-4-yl)oxy)ethanol

22

替卡格雷杂质 W

NA

(1S,2R,3S,4S)-4-(7-chloro-5-(propylthio)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-3-yl)cyclopentane-1,2,3-triol

23

替卡格雷杂质 X

NA

环丙胺片段为（S,S），（R,R）混合物
(1S,2S,3R,5S)-3-(7-(((1R,2R)-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 compound with (1S,2S,3R,5S)-3-(7-(((1S,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 (1:1)

24

替卡瑞洛杂质 Y

376608-65-0

2-(((3aS,4R,6S,6aR)-6-amino-2,2-dimethyltetrahydro-3aH-cyclopenta[d][1,3]dioxol-4-yl)oxy)ethanol (2R,3R)-2,3-dihydroxysuccinate

25

替卡格雷杂质 Z

NA

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

26

替卡格雷工艺中间体杂质1

NA

2-(((3aR,4S,6R,6aS)-6-((5-amino-6-chloro-2-(propylthio)pyrimidin-4-yl)amino)-2,2-dimethyltetrahydro-3aH-cyclopenta[d][1,3]dioxol-4-yl)oxy)ethanol

27

替卡格雷工艺中间体杂质2

NA

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-3aH-cyclopenta[d][1,3]dioxol-4-yl)oxy)ethanol

28

替卡格雷工艺中间体杂质3

NA

2-(((3aR,4S,6R,6aS)-6-((6-chloro-5-nitro-2-(propylthio)pyrimidin-4-yl)amino)-2,2-dimethyltetrahydro-3aH-cyclopenta[d][1,3]dioxol-4-yl)oxy)ethanol

29

替格瑞洛杂质
中间体1脱保护杂质

1354945-69-9

(1S,2S,3R,5S)-3-((5-amino-6-chloro-2-(propylthio)pyrimidin-4-yl)amino)-5-(2-hydroxyethoxy)cyclopentane-1,2-diol

30

替卡格雷API

NA

(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

31

替卡格雷－im A

NA

(1S,2R)-2-(3,4-difluorophenyl)cyclopropanamine

32

替卡格雷－im B

(外消旋体)

NA

(1S,2S)-2-(3,4-difluorophenyl)cyclopropanamine

33

替卡格雷－im C

NA

(1R,2S)-2-(3,4-difluorophenyl)cyclopropanamine

34

替卡格雷－im D

NA

(1R,2S)-2-(3,4-difluorophenyl)cyclopropanamine hydrochloride

35

替卡格雷－im E

NA

1-((1R,2R)-2-(3,4-difluorophenyl)cyclopropyl)-3-((1R,2S)-2-(3,4-difluorophenyl)cyclopropyl)urea

36

替卡格雷－im F

NA

1,3-bis((1R,2S)-2-(3,4-difluorophenyl)cyclopropyl)urea