4-(3-Chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-yl acetate

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CAS:788136-89-0
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CAS:788136-89-0
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CAS:788136-89-0
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CAS:788136-89-0
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4-(3-Chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-yl acetate manufacturers

  • Gefitinib analog III
  • Gefitinib analog III pictures
  • $46.00 / 50mg
  • 2026-05-11
  • CAS:788136-89-0
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  • Purity: 97.60%
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4-(3-Chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-yl acetate Basic information
Product Name:4-(3-Chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-yl acetate
Synonyms:4-[(3-Chloro-4-fluorophenyl)amino]-7-methoxy-6-quinazolinol 6-acetate;4-(3-Chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-yl acetate;6-Quinazolinol,4-[(3-chloro-4-fluorophenyl)amino]-7-methoxy-, 6-acetate;Gefitinib interMediate VI;Gefitinib IMpurity VIII;acetic acid [4-(3-chloro-4-fluoroanilino)-7-methoxy-6-quinazolinyl] ester;4-((3-Chloro-4-fluorophenyl);-7-methoxyquinazolin-6-yl acetate
CAS:788136-89-0
MF:C17H13ClFN3O3
MW:361.75
EINECS:
Product Categories:
Mol File:788136-89-0.mol
4-(3-Chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-yl acetate Structure
4-(3-Chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-yl acetate Chemical Properties
Boiling point 471.5±45.0 °C(Predicted)
density 1.425
storage temp. under inert gas (nitrogen or Argon) at 2–8 °C
pka5.22±0.30(Predicted)
Safety Information
MSDS Information
4-(3-Chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-yl acetate Usage And Synthesis
Uses4-((3-Chloro-4-fluorophenyl)amino)-7-methoxyquinazolin-6-yl Acetate, is an impurity of Gefitinib (G304000), an antineoplastic.
Synthesis
3-Chloro-4-fluoroaniline

367-21-5

6-Acetoxy-4-chloro-7-methoxyquinazoline

230955-75-6

4-(3-Chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-yl acetate

788136-89-0

General procedure for the synthesis of 4-(3-chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-ol acetate from 3-chloro-4-fluoroaniline and 6-acetoxy-4-chloro-7-methoxyquinazoline: at 65°C, AuCl (4.2 g, 18 mmol), 6-acetoxy-4-chloro-7-methoxyquinazoline (12.6 g, 50 mmol) and 3-chloro-4-fluoroaniline (12.3 g, 85 mmol) were dissolved in 50 mL of methanol for substitution reaction. After completion of the reaction, the reaction mixture was filtered. The filtrate was concentrated and washed with petroleum ether to afford 16.9 g of the intermediate 4-(3-chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-ol acetate in 93.4% yield and 99.91% purity.

References[1] Bioorganic and Medicinal Chemistry, 2010, vol. 18, # 2, p. 870 - 879
[2] Patent: CN105693630, 2016, A. Location in patent: Paragraph 0033
[3] Patent: CN106045980, 2016, A. Location in patent: Paragraph 0024; 0025; 0026
[4] Patent: CN108047209, 2018, A. Location in patent: Paragraph 0041; 0047; 0048
[5] Patent: WO2013/71697, 2013, A1. Location in patent: Paragraph 00195
4-(3-Chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-yl acetate Preparation Products And Raw materials
Raw materials3,4-Dihydro-7-methoxy-4-oxoquinazolin-6-yl acetate-->3-Chloro-4-fluoroaniline-->6-Acetoxy-4-chloro-7-methoxyquinazoline-->4-Chloro-3-fluoroaniline-->Methanol-->GOLD (I) CHLORIDE
Preparation ProductsO-Desmorpholinopropyl Gefitinib
Tag:4-(3-Chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-yl acetate(788136-89-0) Related Product Information
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