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1421373-65-0

  • Product NameOsimertinib (AZD9291)
  • Molecular Weight499.616
  • Purity99%
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  • CasNo: 1421373-65-0
  • Purity: 99%

Cost-effective and customizable Osimertinib (AZD9291) 1421373-65-0 in stock

  • Molecular Formula:C28H33N7O2
  • Molecular Weight:499.616
  • PKA:12.68±0.70(Predicted) 
  • PSA:0.00000 
  • Density:1.19±0.1 g/cm3(Predicted) 
  • LogP:0.00000 

1421373-65-0 Relevant articles

Improvements in the Synthesis of the Third-Generation EGFR Inhibitor Osimertinib

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Compound for inhibiting three-mutant epidermal growth factor receptor tyrosine kinase and application thereof

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Paragraph 0039; 0073; 0074; 0090-0092, (2021/09/15)

The invention discloses a compound for i...

AN IMPROVED PROCESS FOR THE PREPARATION OF OSIMERTINIB MESYLATE

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Paragraph 6, (2021/06/11)

The present invention relates to an impr...

Industrial preparation method of AZD9291

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Paragraph 0031-0042, (2021/03/03)

The invention relates to a preparation m...

1421373-65-0 Process route

N?2?[[2?(dimethylamino)ethyl]methylamino]?4?methoxy?5?[[4?(1?methyl?1H?indole-3-yl)-2-pyrimidinyl]amino]aniline
1421372-66-8

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

acryloyl chloride
814-68-6,25189-84-8

acryloyl chloride

[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]
1421373-65-0

[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]

Conditions
Conditions Yield
With sodium carbonate; In N,N-dimethyl-formamide; at -5 ℃; for 2h; Temperature; Solvent;
95.5%
With N-ethyl-N,N-diisopropylamine; In tetrahydrofuran; at 40 ℃; for 12h; Solvent; Reagent/catalyst; Temperature;
88%
With triethylamine; In tetrahydrofuran; at 0 - 20 ℃; for 3h; Temperature; Inert atmosphere;
87%
With triethylamine; In ethyl acetate; at 5 - 10 ℃; Inert atmosphere;
86.37%
With N-ethyl-N,N-diisopropylamine; In dichloromethane; for 1.5h; Cooling with ice;
83%
With triethylamine; In dichloromethane; at 5 - 20 ℃;
79%
With N-ethyl-N,N-diisopropylamine; In chloroform; at 5 - 15 ℃; for 2h; Solvent; Temperature;
72%
With N-ethyl-N,N-diisopropylamine; In chloroform; at 5 - 15 ℃; for 2h; Solvent;
72%
With N-ethyl-N,N-diisopropylamine; In dichloromethane; for 1.5h; Cooling with ice;
57.97%
With N-ethyl-N,N-diisopropylamine; In dichloromethane; at -10 ℃; for 1h;
47%
With N-ethyl-N,N-diisopropylamine; In dichloromethane; for 1.5h; Cooling with ice;
39%
With N-ethyl-N,N-diisopropylamine; In dichloromethane; at 0 ℃; for 1.5h; Inert atmosphere;
39%
N?2?[[2?(dimethylamino)ethyl]methylamino]?4?methoxy?5?[[4?(1?methyl?1H?indole-3-yl)-2-pyrimidinyl]amino]aniline; With N-ethyl-N,N-diisopropylamine; In dichloromethane; at 0 ℃; for 0.0833333h; Inert atmosphere;
acryloyl chloride; In dichloromethane; at 0 ℃; Inert atmosphere;
34.2%
N?2?[[2?(dimethylamino)ethyl]methylamino]?4?methoxy?5?[[4?(1?methyl?1H?indole-3-yl)-2-pyrimidinyl]amino]aniline
1421372-66-8

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

2-chloropropionyl chloride
625-36-5

2-chloropropionyl chloride

[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]
1421373-65-0

[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]

Conditions
Conditions Yield
N?2?[[2?(dimethylamino)ethyl]methylamino]?4?methoxy?5?[[4?(1?methyl?1H?indole-3-yl)-2-pyrimidinyl]amino]aniline; 2-chloropropionyl chloride; With N-ethyl-N,N-diisopropylamine; In tetrahydrofuran; water; at 0 - 20 ℃; for 0.25h;
With sodium hydroxide; In tetrahydrofuran; water; at 65 ℃; for 10h;
94%
N?2?[[2?(dimethylamino)ethyl]methylamino]?4?methoxy?5?[[4?(1?methyl?1H?indole-3-yl)-2-pyrimidinyl]amino]aniline; 2-chloropropionyl chloride; In tetrahydrofuran; water; at 20 ℃; for 0.25h;
With sodium hydroxide; In tetrahydrofuran; water; at 65 ℃; for 10h;
94%
N?2?[[2?(dimethylamino)ethyl]methylamino]?4?methoxy?5?[[4?(1?methyl?1H?indole-3-yl)-2-pyrimidinyl]amino]aniline; 2-chloropropionyl chloride; In tetrahydrofuran; at 0 - 20 ℃; for 0.25h;
With sodium hydroxide; In tetrahydrofuran; at 65 ℃; for 10h;
94%
N?2?[[2?(dimethylamino)ethyl]methylamino]?4?methoxy?5?[[4?(1?methyl?1H?indole-3-yl)-2-pyrimidinyl]amino]aniline; 2-chloropropionyl chloride; In tetrahydrofuran; water; at 0 - 28 ℃; for 1h;
With sodium hydroxide; In tetrahydrofuran; water; for 8h; Reflux;
79.6%
N?2?[[2?(dimethylamino)ethyl]methylamino]?4?methoxy?5?[[4?(1?methyl?1H?indole-3-yl)-2-pyrimidinyl]amino]aniline; 2-chloropropionyl chloride; In water; acetone; at -3 - 30 ℃; for 1.5h;
With triethylamine; In water; acetone; at 25 - 60 ℃;
77.14%

1421373-65-0 Upstream products

  • 1075705-01-9
    1075705-01-9

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

  • 1421372-66-8
    1421372-66-8

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

  • 814-68-6
    814-68-6

    acryloyl chloride

  • 625-36-5
    625-36-5

    2-chloropropionyl chloride

1421373-65-0 Downstream products

  • 1421373-66-1
    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

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