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1421373-66-1

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Basic Information
CAS No.: 1421373-66-1
Name: AZD-9291 (Mesylate)
Article Data: 11
Cas Database
Molecular Structure:
Molecular Structure of 1421373-66-1 (AZD-9291 (Mesylate))
Formula: C29H37N7O5S
Molecular Weight: 595.723
Synonyms: AZD-9291 (Mesylate);N-[2-[[2-(Dimethylamino)ethyl]methylamino]-4-methoxy-5-[[4-(1-methyl-1H-indol-3-yl)-2-pyrimidinyl]amino]phenyl]-2-propenamide methanesulfonate (1:1);AZD-9291 mesylate N-[2-[[2-(Dimethylamino)ethyl]methylamino]-4-methoxy-5-[[4-(1-methyl-1H-indol-3-yl)-2-pyrimidinyl]amino]phenyl]-2-propenamide methanesulfonate (1:1);Osimertinib mesylate;Mereletinib mesylate;Osimertinib;N-[2-(2-dimethylaminoethylmethylamino)-4-methoxy-5-[[4-(1-methylindol-3-yl)pyrimidin-2-yl]amino]phenyl]prop-2-enamide mesylate salt;Osimertinib Mesylate(AZD9291)
EINECS: 200-064-1
Density: N/A
Melting Point: N/A
Boiling Point: N/A
Flash Point: N/A
Solubility: N/A
Appearance: N/A
Hazard Symbols: N/A
Risk Codes: N/A
Safety:
Transport Information: N/A
PSA: 153.79000
LogP: 5.81710
Related products
Synthetic route
75-75-2

methanesulfonic acid

1421373-65-0

[N-(2-{[2-(dimethylamino)ethyl](methyl)amino}-4-methoxy-5-{[4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl]amino}phenyl)propen-2-amide]

1421373-66-1

N-(2-(N-(2-(dimethylamino)ethyl)-N-methylamino)-4-methoxy-5-((4-(1-methyl-1H-indole-3-yl)pyrimidine-2-yl)amino)phenyl)acrylamide methanesulfonate

Conditions
ConditionsYield
Stage #1: [N-(2-{[2-(dimethylamino)ethyl](methyl)amino}-4-methoxy-5-{[4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl]amino}phenyl)propen-2-amide] With pyrographite In acetone at 25 - 55℃;
Stage #2: methanesulfonic acid at 25 - 55℃;		96.73%
With N-ethyl-N,N-diisopropylamine In ethanol; ethyl acetate at 70℃; for 1.5h;94%
In water; acetone at 50℃; for 1.5h; Inert atmosphere;94%
1075705-01-9

4-fluoro-2-methoxy-5-nitro-phenylamine

1421373-66-1

N-(2-(N-(2-(dimethylamino)ethyl)-N-methylamino)-4-methoxy-5-((4-(1-methyl-1H-indole-3-yl)pyrimidine-2-yl)amino)phenyl)acrylamide methanesulfonate

Conditions
ConditionsYield
Multi-step reaction with 5 steps
1.1: toluene-4-sulfonic acid / 2.5 h / 105 °C
2.1: N-ethyl-N,N-diisopropylamine / N,N-dimethyl acetamide / 85 °C
3.1: iron; ammonium chloride / water; ethanol / 2 h / Reflux
4.1: N-ethyl-N,N-diisopropylamine / water; tetrahydrofuran / 0.25 h / 0 - 20 °C
4.2: 10 h / 65 °C
5.1: N-ethyl-N,N-diisopropylamine / ethyl acetate; ethanol / 1.5 h / 70 °C
View Scheme
Multi-step reaction with 5 steps
1: toluene-4-sulfonic acid / 2.5 h / 105 °C
2: N-ethyl-N,N-diisopropylamine / N,N-dimethyl acetamide / 85 °C
3: iron; ammonium chloride / water; ethanol / 2 h / Reflux
4: N-ethyl-N,N-diisopropylamine / dichloromethane / 1.5 h / Cooling with ice
5: N-ethyl-N,N-diisopropylamine / ethyl acetate; ethanol / 1.5 h / 70 °C
View Scheme
Multi-step reaction with 6 steps
1: toluene-4-sulfonic acid / 2.5 h / 105 °C
2: N-ethyl-N,N-diisopropylamine / N,N-dimethyl acetamide / 85 °C
3: iron; ammonium chloride / water; ethanol / 2 h / Reflux
4: potassium carbonate / acetone / 0.5 h / -50 - -20 °C
5: triethylamine / acetonitrile / 6 h / 80 °C
6: N-ethyl-N,N-diisopropylamine / ethyl acetate; ethanol / 1.5 h / 70 °C
View Scheme
1421372-66-8

N‑2‑[[2‑(dimethylamino)ethyl]methylamino]‑4‑methoxy‑5‑[[4‑(1‑methyl‑1H‑indole-3-yl)-2-pyrimidinyl]amino]aniline

1421373-66-1

N-(2-(N-(2-(dimethylamino)ethyl)-N-methylamino)-4-methoxy-5-((4-(1-methyl-1H-indole-3-yl)pyrimidine-2-yl)amino)phenyl)acrylamide methanesulfonate

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1.1: N-ethyl-N,N-diisopropylamine / water; tetrahydrofuran / 0.25 h / 0 - 20 °C
1.2: 10 h / 65 °C
2.1: N-ethyl-N,N-diisopropylamine / ethyl acetate; ethanol / 1.5 h / 70 °C
View Scheme
Multi-step reaction with 2 steps
1: N-ethyl-N,N-diisopropylamine / dichloromethane / 1.5 h / Cooling with ice
2: N-ethyl-N,N-diisopropylamine / ethyl acetate; ethanol / 1.5 h / 70 °C
View Scheme
Multi-step reaction with 3 steps
1: potassium carbonate / acetone / 0.5 h / -50 - -20 °C
2: triethylamine / acetonitrile / 6 h / 80 °C
3: N-ethyl-N,N-diisopropylamine / ethyl acetate; ethanol / 1.5 h / 70 °C
View Scheme
1421372-67-9

N1-(2-(dimethylamino)ethyl)-5-methoxy-N1-methyl-N4-(4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)-2-nitrobenzene-1,4-diamine

1421373-66-1

N-(2-(N-(2-(dimethylamino)ethyl)-N-methylamino)-4-methoxy-5-((4-(1-methyl-1H-indole-3-yl)pyrimidine-2-yl)amino)phenyl)acrylamide methanesulfonate

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1.1: iron; ammonium chloride / water; ethanol / 2 h / Reflux
2.1: N-ethyl-N,N-diisopropylamine / water; tetrahydrofuran / 0.25 h / 0 - 20 °C
2.2: 10 h / 65 °C
3.1: N-ethyl-N,N-diisopropylamine / ethyl acetate; ethanol / 1.5 h / 70 °C
View Scheme
Multi-step reaction with 3 steps
1: iron; ammonium chloride / water; ethanol / 2 h / Reflux
2: N-ethyl-N,N-diisopropylamine / dichloromethane / 1.5 h / Cooling with ice
3: N-ethyl-N,N-diisopropylamine / ethyl acetate; ethanol / 1.5 h / 70 °C
View Scheme
Multi-step reaction with 4 steps
1: iron; ammonium chloride / water; ethanol / 2 h / Reflux
2: potassium carbonate / acetone / 0.5 h / -50 - -20 °C
3: triethylamine / acetonitrile / 6 h / 80 °C
4: N-ethyl-N,N-diisopropylamine / ethyl acetate; ethanol / 1.5 h / 70 °C
View Scheme
1421372-94-2

N-(4-fluoro-2-methoxy-5-nitrophenyl)-4-(1-methyl-1H-indole-3-yl)-pyrimidine-2-amine

1421373-66-1

N-(2-(N-(2-(dimethylamino)ethyl)-N-methylamino)-4-methoxy-5-((4-(1-methyl-1H-indole-3-yl)pyrimidine-2-yl)amino)phenyl)acrylamide methanesulfonate

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1.1: N-ethyl-N,N-diisopropylamine / N,N-dimethyl acetamide / 85 °C
2.1: iron; ammonium chloride / water; ethanol / 2 h / Reflux
3.1: N-ethyl-N,N-diisopropylamine / water; tetrahydrofuran / 0.25 h / 0 - 20 °C
3.2: 10 h / 65 °C
4.1: N-ethyl-N,N-diisopropylamine / ethyl acetate; ethanol / 1.5 h / 70 °C
View Scheme
Multi-step reaction with 4 steps
1: N-ethyl-N,N-diisopropylamine / N,N-dimethyl acetamide / 85 °C
2: iron; ammonium chloride / water; ethanol / 2 h / Reflux
3: N-ethyl-N,N-diisopropylamine / dichloromethane / 1.5 h / Cooling with ice
4: N-ethyl-N,N-diisopropylamine / ethyl acetate; ethanol / 1.5 h / 70 °C
View Scheme
Multi-step reaction with 5 steps
1: N-ethyl-N,N-diisopropylamine / N,N-dimethyl acetamide / 85 °C
2: iron; ammonium chloride / water; ethanol / 2 h / Reflux
3: potassium carbonate / acetone / 0.5 h / -50 - -20 °C
4: triethylamine / acetonitrile / 6 h / 80 °C
5: N-ethyl-N,N-diisopropylamine / ethyl acetate; ethanol / 1.5 h / 70 °C
View Scheme
1032452-86-0

2-chloro-4-(1'-methyl-1H-indol-3-yl)pyrimidine

1421373-66-1

N-(2-(N-(2-(dimethylamino)ethyl)-N-methylamino)-4-methoxy-5-((4-(1-methyl-1H-indole-3-yl)pyrimidine-2-yl)amino)phenyl)acrylamide methanesulfonate

Conditions
ConditionsYield
Multi-step reaction with 5 steps
1.1: toluene-4-sulfonic acid / 2.5 h / 105 °C
2.1: N-ethyl-N,N-diisopropylamine / N,N-dimethyl acetamide / 85 °C
3.1: iron; ammonium chloride / water; ethanol / 2 h / Reflux
4.1: N-ethyl-N,N-diisopropylamine / water; tetrahydrofuran / 0.25 h / 0 - 20 °C
4.2: 10 h / 65 °C
5.1: N-ethyl-N,N-diisopropylamine / ethyl acetate; ethanol / 1.5 h / 70 °C
View Scheme
Multi-step reaction with 5 steps
1: toluene-4-sulfonic acid / 2.5 h / 105 °C
2: N-ethyl-N,N-diisopropylamine / N,N-dimethyl acetamide / 85 °C
3: iron; ammonium chloride / water; ethanol / 2 h / Reflux
4: N-ethyl-N,N-diisopropylamine / dichloromethane / 1.5 h / Cooling with ice
5: N-ethyl-N,N-diisopropylamine / ethyl acetate; ethanol / 1.5 h / 70 °C
View Scheme
Multi-step reaction with 6 steps
1: toluene-4-sulfonic acid / 2.5 h / 105 °C
2: N-ethyl-N,N-diisopropylamine / N,N-dimethyl acetamide / 85 °C
3: iron; ammonium chloride / water; ethanol / 2 h / Reflux
4: potassium carbonate / acetone / 0.5 h / -50 - -20 °C
5: triethylamine / acetonitrile / 6 h / 80 °C
6: N-ethyl-N,N-diisopropylamine / ethyl acetate; ethanol / 1.5 h / 70 °C
View Scheme
945016-63-7

3-(2-chloro-pyrimidin-4-yl)-1H-indole

1421373-66-1

N-(2-(N-(2-(dimethylamino)ethyl)-N-methylamino)-4-methoxy-5-((4-(1-methyl-1H-indole-3-yl)pyrimidine-2-yl)amino)phenyl)acrylamide methanesulfonate

Conditions
ConditionsYield
Multi-step reaction with 6 steps
1.1: sodium hydride / tetrahydrofuran; mineral oil / 0.5 h / 0 °C
1.2: 3 h / 0 °C
2.1: toluene-4-sulfonic acid / 2.5 h / 105 °C
3.1: N-ethyl-N,N-diisopropylamine / N,N-dimethyl acetamide / 85 °C
4.1: iron; ammonium chloride / water; ethanol / 2 h / Reflux
5.1: N-ethyl-N,N-diisopropylamine / water; tetrahydrofuran / 0.25 h / 0 - 20 °C
5.2: 10 h / 65 °C
6.1: N-ethyl-N,N-diisopropylamine / ethyl acetate; ethanol / 1.5 h / 70 °C
View Scheme
Multi-step reaction with 6 steps
1.1: sodium hydride / tetrahydrofuran; mineral oil / 0.5 h / 0 °C
1.2: 3 h / 0 °C
2.1: toluene-4-sulfonic acid / 2.5 h / 105 °C
3.1: N-ethyl-N,N-diisopropylamine / N,N-dimethyl acetamide / 85 °C
4.1: iron; ammonium chloride / water; ethanol / 2 h / Reflux
5.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 1.5 h / Cooling with ice
6.1: N-ethyl-N,N-diisopropylamine / ethyl acetate; ethanol / 1.5 h / 70 °C
View Scheme
Multi-step reaction with 7 steps
1.1: sodium hydride / tetrahydrofuran; mineral oil / 0.5 h / 0 °C
1.2: 3 h / 0 °C
2.1: toluene-4-sulfonic acid / 2.5 h / 105 °C
3.1: N-ethyl-N,N-diisopropylamine / N,N-dimethyl acetamide / 85 °C
4.1: iron; ammonium chloride / water; ethanol / 2 h / Reflux
5.1: potassium carbonate / acetone / 0.5 h / -50 - -20 °C
6.1: triethylamine / acetonitrile / 6 h / 80 °C
7.1: N-ethyl-N,N-diisopropylamine / ethyl acetate; ethanol / 1.5 h / 70 °C
View Scheme
Multi-step reaction with 6 steps
1.1: sodium hydride / tetrahydrofuran / 0.5 h / 0 °C / Inert atmosphere
1.2: 3 h / 0 °C / Inert atmosphere
2.1: toluene-4-sulfonic acid / 2.5 h / 105 °C / Inert atmosphere
3.1: N-ethyl-N,N-diisopropylamine / 2,2,2-trifluoroethanol / 1 h / 140 °C / Inert atmosphere
4.1: ammonium chloride; iron / ethanol; water / 2 h / 100 °C / Inert atmosphere
5.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 1.5 h / 0 °C / Inert atmosphere
6.1: water; acetone / 1.5 h / 50 °C / Inert atmosphere
View Scheme
1421373-36-5

3-chloro-N-(2-{[2-(dimethylamino)ethyl](methyl)amino}-4-methoxy-5-{[4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl]amino}phenyl)propanamide

1421373-66-1

N-(2-(N-(2-(dimethylamino)ethyl)-N-methylamino)-4-methoxy-5-((4-(1-methyl-1H-indole-3-yl)pyrimidine-2-yl)amino)phenyl)acrylamide methanesulfonate

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1: triethylamine / acetonitrile / 6 h / 80 °C
2: N-ethyl-N,N-diisopropylamine / ethyl acetate; ethanol / 1.5 h / 70 °C
View Scheme
Multi-step reaction with 2 steps
1: sodium hydroxide / tetrahydrofuran; water / 10 h / 65 °C
2: water; ethanol / 1.5 h / 70 °C
View Scheme
120-72-9

indole

1421373-66-1

N-(2-(N-(2-(dimethylamino)ethyl)-N-methylamino)-4-methoxy-5-((4-(1-methyl-1H-indole-3-yl)pyrimidine-2-yl)amino)phenyl)acrylamide methanesulfonate

Conditions
ConditionsYield
Multi-step reaction with 7 steps
1.1: methylmagnesium bromide / diethyl ether; 1,2-dichloro-ethane / 0.42 h / 0 °C / Inert atmosphere
1.2: 16 h / 0 - 20 °C / Inert atmosphere
2.1: sodium hydride / tetrahydrofuran; mineral oil / 0.5 h / 0 °C
2.2: 3 h / 0 °C
3.1: toluene-4-sulfonic acid / 2.5 h / 105 °C
4.1: N-ethyl-N,N-diisopropylamine / N,N-dimethyl acetamide / 85 °C
5.1: iron; ammonium chloride / water; ethanol / 2 h / Reflux
6.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 1.5 h / Cooling with ice
7.1: N-ethyl-N,N-diisopropylamine / ethyl acetate; ethanol / 1.5 h / 70 °C
View Scheme
Multi-step reaction with 7 steps
1.1: methylmagnesium bromide / diethyl ether; 1,2-dichloro-ethane / 0.42 h / 0 °C / Inert atmosphere
1.2: 16 h / 0 - 20 °C / Inert atmosphere
2.1: sodium hydride / tetrahydrofuran; mineral oil / 0.5 h / 0 °C
2.2: 3 h / 0 °C
3.1: toluene-4-sulfonic acid / 2.5 h / 105 °C
4.1: N-ethyl-N,N-diisopropylamine / N,N-dimethyl acetamide / 85 °C
5.1: iron; ammonium chloride / water; ethanol / 2 h / Reflux
6.1: N-ethyl-N,N-diisopropylamine / water; tetrahydrofuran / 0.25 h / 0 - 20 °C
6.2: 10 h / 65 °C
7.1: N-ethyl-N,N-diisopropylamine / ethyl acetate; ethanol / 1.5 h / 70 °C
View Scheme
Multi-step reaction with 8 steps
1.1: methylmagnesium bromide / diethyl ether; 1,2-dichloro-ethane / 0.42 h / 0 °C / Inert atmosphere
1.2: 16 h / 0 - 20 °C / Inert atmosphere
2.1: sodium hydride / tetrahydrofuran; mineral oil / 0.5 h / 0 °C
2.2: 3 h / 0 °C
3.1: toluene-4-sulfonic acid / 2.5 h / 105 °C
4.1: N-ethyl-N,N-diisopropylamine / N,N-dimethyl acetamide / 85 °C
5.1: iron; ammonium chloride / water; ethanol / 2 h / Reflux
6.1: potassium carbonate / acetone / 0.5 h / -50 - -20 °C
7.1: triethylamine / acetonitrile / 6 h / 80 °C
8.1: N-ethyl-N,N-diisopropylamine / ethyl acetate; ethanol / 1.5 h / 70 °C
View Scheme
Multi-step reaction with 7 steps
1.1: methylmagnesium bromide / diethyl ether; 1,2-dichloro-ethane / 0.25 h / 0 °C / Inert atmosphere
1.2: 16 h / 0 °C / Inert atmosphere; Heating
2.1: sodium hydride / tetrahydrofuran / 0.5 h / 0 °C / Inert atmosphere
2.2: 3 h / 0 °C / Inert atmosphere
3.1: toluene-4-sulfonic acid / 2.5 h / 105 °C / Inert atmosphere
4.1: N-ethyl-N,N-diisopropylamine / 2,2,2-trifluoroethanol / 1 h / 140 °C / Inert atmosphere
5.1: ammonium chloride; iron / ethanol; water / 2 h / 100 °C / Inert atmosphere
6.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 1.5 h / 0 °C / Inert atmosphere
7.1: water; acetone / 1.5 h / 50 °C / Inert atmosphere
View Scheme
450-91-9

4-fluoro-2-methoxyaniline

1421373-66-1

N-(2-(N-(2-(dimethylamino)ethyl)-N-methylamino)-4-methoxy-5-((4-(1-methyl-1H-indole-3-yl)pyrimidine-2-yl)amino)phenyl)acrylamide methanesulfonate

Conditions
ConditionsYield
Multi-step reaction with 6 steps
1.1: sulfuric acid; potassium nitrate / 15 °C / Cooling with ice
2.1: toluene-4-sulfonic acid / 2.5 h / 105 °C
3.1: N-ethyl-N,N-diisopropylamine / N,N-dimethyl acetamide / 85 °C
4.1: iron; ammonium chloride / water; ethanol / 2 h / Reflux
5.1: N-ethyl-N,N-diisopropylamine / water; tetrahydrofuran / 0.25 h / 0 - 20 °C
5.2: 10 h / 65 °C
6.1: N-ethyl-N,N-diisopropylamine / ethyl acetate; ethanol / 1.5 h / 70 °C
View Scheme
Multi-step reaction with 6 steps
1: sulfuric acid; potassium nitrate / 15 °C / Cooling with ice
2: toluene-4-sulfonic acid / 2.5 h / 105 °C
3: N-ethyl-N,N-diisopropylamine / N,N-dimethyl acetamide / 85 °C
4: iron; ammonium chloride / water; ethanol / 2 h / Reflux
5: N-ethyl-N,N-diisopropylamine / dichloromethane / 1.5 h / Cooling with ice
6: N-ethyl-N,N-diisopropylamine / ethyl acetate; ethanol / 1.5 h / 70 °C
View Scheme
Multi-step reaction with 7 steps
1: sulfuric acid; potassium nitrate / 15 °C / Cooling with ice
2: toluene-4-sulfonic acid / 2.5 h / 105 °C
3: N-ethyl-N,N-diisopropylamine / N,N-dimethyl acetamide / 85 °C
4: iron; ammonium chloride / water; ethanol / 2 h / Reflux
5: potassium carbonate / acetone / 0.5 h / -50 - -20 °C
6: triethylamine / acetonitrile / 6 h / 80 °C
7: N-ethyl-N,N-diisopropylamine / ethyl acetate; ethanol / 1.5 h / 70 °C
View Scheme
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    FOB Price:  USD $ 10.0-10.0/Gram

    We promise our customer following items 1.Reasonable price: We provide high quality products with competitive price in china, 2.Low moq: No worry about the low moq, our moq is 1 gram or lower. 3.Good and efficient service,Fast Delivery Fast res

    Xi’an JunYuan Biotech Co., Ltd., which is specialized in fine chemicals research, production and sales. It has strong professional research and development team, talented personne

  •  XI'AN JUNYUAN BIO-TECH CO., LTD.

     China (Mainland)  |  Contact Details

    Business Type:Trading Company

    Tel:+86-29-86106815

    Address:Block C of XINJIE, No. 398, Fengcheng 6 Road, Xi'an Economic & Technological Development Zone

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