314771-88-5

  • Product Name:4-QuinazolinaMine, N-(3-chloro-4-fluorophenyl)-6-nitro-7-[[(3S)-tetrahydro-3-furanyl]oxy]-
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Product Details

Purity:99%

High Quality 314771-88-5 Fast Delivery (4-QuinazolinaMine, N-(3-chloro-4-fluorophenyl)-6-nitro-7-[[(3S)-tetrahydro-3-furanyl]oxy]-)

  • Molecular Formula:C18H14ClFN4O4
  • Molecular Weight:404.78000
  • Boiling Point:585.0±50.0 °C(Predicted) 
  • PKA:5.07±0.70(Predicted) 
  • PSA:102.09000 
  • Density:1.534±0.06 g/cm3(Predicted) 
  • LogP:4.83800 

4-QuinazolinaMine, N-(3-chloro-4-fluorophenyl)-6-nitro-7-[[(3S)-tetrahydro-3-furanyl]oxy]-(Cas 314771-88-5) Usage

Uses

(S)-N-(3-chloro-4-fluorophenyl)-6-nitro-7-(tetrahydrofuran-3-yloxy)quinazolin-4-amine is a used in the synthetic preparation of 4-anilinoquinazolines with C-6 urea-linked side chains as inhibitors of epidermal growth factor receptor. It is also used in the preparation of (2Z)-Afatinib (A355305) which is used for treating cancer and diseases of the respiratory tract, lungs, gastrointestinal tract, bile duct, and gallbladder.

 

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PROCESS FOR THE PREPARATION OF N-[4-[(3-CHLORO-4-FLUORO PHENYL) AMINO]-7-[[(3s-TETRAHYDRO-3-FURANYL]OXY]-6-QUINAZOLINYL]-4-(DIMETHYL AMINO)-(2E)-2-BUTENAMIDE (2Z)-2-BUTENEDIOATE (1 :2) AND ITS POLYMORPHS THEREOF

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, (2018/11/21)

The present invention relates to an impr...

314771-88-5 Process route

N-((3-chloro-4-fluorophenyl)-6-nitro-7-phenylsulfonyl)quinazolin-4-one
945553-94-6

N-((3-chloro-4-fluorophenyl)-6-nitro-7-phenylsulfonyl)quinazolin-4-one

(S)-3-hydroxytetyrahydrofurane
86087-23-2,84921-89-1,864447-89-2

(S)-3-hydroxytetyrahydrofurane

4-[(3-chloro-4-fluorophenyl)amino]-6-nitro-7-[(S)-(tetrahydrofuran-3-yl)oxy]quinazoline
314771-88-5,402855-07-6

4-[(3-chloro-4-fluorophenyl)amino]-6-nitro-7-[(S)-(tetrahydrofuran-3-yl)oxy]quinazoline

Conditions
Conditions Yield
With potassium tert-butylate; In tetrahydrofuran; N,N-dimethyl-formamide; tert-butyl alcohol; at 20 - 45 ℃; for 8h;
89.6%
With sodium hydride; In N,N-dimethyl-formamide; at 0 - 20 ℃; for 4h;
 
7-chloro-6-nitro-4(3H)-quinazolinone
53449-14-2

7-chloro-6-nitro-4(3H)-quinazolinone

4-[(3-chloro-4-fluorophenyl)amino]-6-nitro-7-[(S)-(tetrahydrofuran-3-yl)oxy]quinazoline
314771-88-5,402855-07-6

4-[(3-chloro-4-fluorophenyl)amino]-6-nitro-7-[(S)-(tetrahydrofuran-3-yl)oxy]quinazoline

Conditions
Conditions Yield
Multi-step reaction with 4 steps
1: trichlorophosphate / 2 h / 90 °C
2: 1,4-dioxane / 3 h / 90 °C
3: 2 h / 90 °C
4: sodium hydride / N,N-dimethyl-formamide / 4 h / 0 - 20 °C
With sodium hydride; trichlorophosphate; In 1,4-dioxane; N,N-dimethyl-formamide;
 
Multi-step reaction with 2 steps
1.1: thionyl chloride / N,N-dimethyl-formamide / 3 h / Reflux
1.2: 1 h / 90 °C
2.1: potassium tert-butylate / N,N-dimethyl-formamide / 2 h / 0 °C
2.2: 6 h / 30 - 90 °C
With thionyl chloride; potassium tert-butylate; In N,N-dimethyl-formamide;
 

314771-88-5 Upstream products

  • 945553-94-6
    945553-94-6

    N-((3-chloro-4-fluorophenyl)-6-nitro-7-phenylsulfonyl)quinazolin-4-one

  • 86087-23-2
    86087-23-2

    (S)-3-hydroxytetyrahydrofurane

  • 367-21-5
    367-21-5

    3-chloro-4-fluorophenylamine

  • 162012-67-1
    162012-67-1

    N-(3-chloro-4-fluorophenyl)-7-fluoro-6-nitroquinazolin-4-amine

314771-88-5 Downstream products

  • 314771-76-1
    314771-76-1

    6-Amino-4-[(3-chloro-4-fluorophenyl)amino]-7-[(S)-(tetrahydrofuran-3-yl)oxy]quinazoline