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
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
Safety
- HS Code
- 2933.59.8000
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.
N-Bromosuccinimide Price
- Product number
- C3276
- Product name
- N-(3-Chloro-4-fluorophenyl)-7-fluoro-6-nitro-4-quinazolinamine
- Packaging
- 5G
- Price
- $147
- Updated
- 2025/07/31
- Product number
- C3276
- Product name
- N-(3-Chloro-4-fluorophenyl)-7-fluoro-6-nitro-4-quinazolinamine
- Packaging
- 25G
- Price
- $437
- Updated
- 2025/07/31
- Product number
- C376250
- Product name
- 4-(3-Chloro-4-fluorophenylamino)-7-fluoro-6-nitroquinazoline
- Packaging
- 10g
- Price
- $970
- Updated
- 2021/12/16
- Product number
- C376250
- Product name
- 4-(3-Chloro-4-fluorophenylamino)-7-fluoro-6-nitroquinazoline
- Packaging
- 100mg
- Price
- $95
- Updated
- 2021/12/16
- Product number
- B693
- Product name
- 4-(3-Chloro-4-fluorophenylamino)-7-fluoro-6-nitroquninazoline
- Packaging
- 5g
- Price
- $98
- Updated
- 2021/12/16
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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View Lastest Price from 4-Quinazolinamine, N-(3-chloro-4-fluorophenyl)-7-fluoro-6-nitro- manufacturers
- 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
- 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
- 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