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Purity:99%
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. |
The present invention relates to a high ...
The invention discloses an afatinib refi...
A series of quinazoline derivatives with...
The present invention relates to an impr...
N-((3-chloro-4-fluorophenyl)-6-nitro-7-phenylsulfonyl)quinazolin-4-one
(S)-3-hydroxytetyrahydrofurane
4-[(3-chloro-4-fluorophenyl)amino]-6-nitro-7-[(S)-(tetrahydrofuran-3-yl)oxy]quinazoline
Conditions | Yield |
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With potassium tert-butylate; In tetrahydrofuran; N,N-dimethyl-formamide; tert-butyl alcohol; at 20 - 45 ℃; for 8h;
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89.6% |
With sodium hydride; In N,N-dimethyl-formamide; at 0 - 20 ℃; for 4h;
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7-chloro-6-nitro-4(3H)-quinazolinone
4-[(3-chloro-4-fluorophenyl)amino]-6-nitro-7-[(S)-(tetrahydrofuran-3-yl)oxy]quinazoline
Conditions | Yield |
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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;
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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;
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N-((3-chloro-4-fluorophenyl)-6-nitro-7-phenylsulfonyl)quinazolin-4-one
(S)-3-hydroxytetyrahydrofurane
3-chloro-4-fluorophenylamine
N-(3-chloro-4-fluorophenyl)-7-fluoro-6-nitroquinazolin-4-amine
6-Amino-4-[(3-chloro-4-fluorophenyl)amino]-7-[(S)-(tetrahydrofuran-3-yl)oxy]quinazoline