ChemicalBook > CAS DataBase List > 4-Quinazolinamine, N-(3-chloro-4-fluorophenyl)-7-fluoro-6-nitro-

4-Quinazolinamine, N-(3-chloro-4-fluorophenyl)-7-fluoro-6-nitro-

Product Name
4-Quinazolinamine, N-(3-chloro-4-fluorophenyl)-7-fluoro-6-nitro-
CAS No.
162012-67-1
Chemical Name
4-Quinazolinamine, N-(3-chloro-4-fluorophenyl)-7-fluoro-6-nitro-
Synonyms
N-(3-chloro-4-fluorophenyl)-7-fluoro-6-nitroquinazolin-4-amine;4-(3-chloro-4-fiuoro-phenylaMino)-7-fluoro-6-nitroquninazoline;N-(3-Chloro-4-fluorophenyl)-7-fluoro-6-nitro-4-quinazolinamine;N-(4-(3-chloro-4-fluorophenyl))-7-fluoro-6nitroquinazolin-4-amine;)-7-fL;Afatinib Impurity 76;Afatinib/Dacomitinib;uoro-6-nitroquninazoL;Afatinib Impurity 114;Afatinib intermediate A
CBNumber
CB41512555
Molecular Formula
C14H7ClF2N4O2
Formula Weight
336.68
MOL File
162012-67-1.mol
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4-Quinazolinamine, N-(3-chloro-4-fluorophenyl)-7-fluoro-6-nitro- Property

Melting point:
242-244℃
Boiling point:
489℃
Density 
1.616
Flash point:
249℃
storage temp. 
2-8°C(protect from light)
solubility 
DMSO (Slightly), Methanol (Slightly, Sonicated)
form 
Solid
pka
5.07±0.70(Predicted)
color 
Yellow to Dark Yellow
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Safety

HS Code 
2933.59.8000
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P362Take off contaminated clothing and wash before reuse.

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N-Bromosuccinimide Price

TCI Chemical
Product number
C3276
Product name
N-(3-Chloro-4-fluorophenyl)-7-fluoro-6-nitro-4-quinazolinamine
Packaging
5G
Price
$147
Updated
2025/07/31
TCI Chemical
Product number
C3276
Product name
N-(3-Chloro-4-fluorophenyl)-7-fluoro-6-nitro-4-quinazolinamine
Packaging
25G
Price
$437
Updated
2025/07/31
TRC
Product number
C376250
Product name
4-(3-Chloro-4-fluorophenylamino)-7-fluoro-6-nitroquinazoline
Packaging
100mg
Price
$95
Updated
2021/12/16
TRC
Product number
C376250
Product name
4-(3-Chloro-4-fluorophenylamino)-7-fluoro-6-nitroquinazoline
Packaging
10g
Price
$970
Updated
2021/12/16
ChemScene
Product number
CS-M0991
Product name
N-(3-chloro-4-fluorophenyl)-7-fluoro-6-nitroquinazolin-4-amine
Purity
>99.0%
Packaging
10g
Price
$32
Updated
2021/12/16
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4-Quinazolinamine, N-(3-chloro-4-fluorophenyl)-7-fluoro-6-nitro- Chemical Properties,Usage,Production

Uses

4-(3-Chloro-4-fluorophenylamino)-7-fluoro-6-nitroquninazoline is an intermediate in the synthesis of Afatinib (A355300), an aminocrotonylamino-substituted quinazoline derivative used for treating cancer and diseases of the respiratory tract, lungs, gastrointestinal tract, bile duct, and gallbladder.

Synthesis

162012-69-3

367-21-5

162012-67-1

The general procedure for the synthesis of N-(3-chloro-4-fluorophenyl)-7-fluoro-6-nitro-4-quinazolinamine from 7-fluoro-6-nitro-4-hydroxyquinazoline and 3-chloro-4-fluoroaniline is as follows: Method 1 (one-pot reaction): 1. 7-fluoro-6-nitro-4-hydroxyquinazoline (5 g, 23.9 mmol) was added to a 100 mL single neck flask. 2. Phosphoryl chloride (44.6 mL, 478 mmol) was added and heated to reflux at 150 °C for 5 hours. 3. Upon completion of the reaction, phosphorous trichloride was removed by evaporation. 4. The residue was diluted with anhydrous dichloromethane and evaporated again, and the process was repeated 3 times. 5. After dilution with acetonitrile (100 mL), 3-chloro-4-fluoroaniline (2.3 g, 15.8 mmol) was added. 6. 6. Heat to reflux overnight and a yellow solid precipitated during the reaction. 7. The yellow solid was filtered and dried to afford the target product N-(3-chloro-4-fluorophenyl)-7-fluoro-6-nitro-4-quinazolinamine (4.8 g, 56% yield). Product characterization data: 1H-NMR (d-DMSO, 400 MHz, δppm): 10.61 (br, 1H), 9.68 (d, J=10.8 Hz, 1H), 8.81 (s, 1H), 8.10-8.13 (d, J=7.6 Hz, 1H), 8.05-8.07 (d, J=8 Hz, 1H), 7.81-7.85 (m. 1H), 7.50-7.54 (d, J=8Hz, 1H).

References

[1] Patent: EP3181553, 2017, A1. Location in patent: Paragraph 0123; 0124

4-Quinazolinamine, N-(3-chloro-4-fluorophenyl)-7-fluoro-6-nitro- Preparation Products And Raw materials

Raw materials

Preparation Products

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4-Quinazolinamine, N-(3-chloro-4-fluorophenyl)-7-fluoro-6-nitro- Suppliers

TOKYO CHEMICAL INDUSTRY CO., LTD.
Tel
03-36680489
Fax
03-3668-0520
Email
Sales-JP@TCIchemicals.com
Country
Japan
ProdList
28387
Advantage
80
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View Lastest Price from 4-Quinazolinamine, N-(3-chloro-4-fluorophenyl)-7-fluoro-6-nitro- manufacturers

Moxin Chemicals
Product
Afatinib Impurity 162012-67-1
Price
US $0.00-0.00/mg
Min. Order
10mg
Purity
99%+ HPLC
Supply Ability
1000
Release date
2025-06-04
Henan Aochuang Chemical Co.,Ltd.
Product
4-Quinazolinamine, N-(3-chloro-4-fluorophenyl)-7-fluoro-6-nitro- 162012-67-1
Price
US $0.00-0.00/kg
Min. Order
1kg
Purity
98%
Supply Ability
1Ton
Release date
2022-09-30
Hebei Yanxi Chemical Co., Ltd.
Product
N-(3-Chloro-4-fluorophenyl)-7-fluoro-6-nitroquinazolin-4-amine 162012-67-1
Price
US $50.00/kg
Min. Order
1kg
Purity
0.99
Supply Ability
20 tons
Release date
2023-09-06

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