The Assessors of the Asian University Network - Quality Assurance (AUN-QA) are warmly welcomed!
Welcome to the Vietnamese Doctors’ Day!
Research / Publications
Synthesis of (S)-N-(3-chloro-4-fluorophenyl)-6-nitro-7-((tetrahydrofuran-3-yl)oxy)quinazolin-4-amine as an important intermediate for the preparation of afatinib
Home Research Publications Synthesis of (S)-N-(3-chloro-4-fluorophenyl)-6-nitro-7-((tetrahydrofuran-3-yl)oxy)quinazolin-4-amine as an important intermediate for the preparation of afatinib

Synthesis of (S)-N-(3-chloro-4-fluorophenyl)-6-nitro-7-((tetrahydrofuran-3-yl)oxy)quinazolin-4-amine as an important intermediate for the preparation of afatinib

T N. N., V H. N., May-2022, In: Journal of Chemistry and Application, 60B, 1B, p. 299-234

Overview

Abstract:

Afatinib is an anti-cancer drug approved for the first-line treatment of EGFR mutation-positive non-small cell lung cancer (NSCLC). The current paper reports for the first time in Vietnam an efficient and convenient synthesis of (S)-N-(3-chloro-4-fluorophenyl)-6-nitro-7-((tetrahydrofuran-3-yl) oxy)quinazolin-4-amine (IV) as an important ether intermediate for preparing this drug. The synthesis was carried out by 2 methods: from aryl sulfone and from aryl fluoride. The process from aryl sulfon was chosen to perform at a scale of 20 g / batch with the good yield of 86.1%. This process has the advantages of mild reaction conditions, simple operation and low cost, which is useful for further optimizing and developing synthesis process of afatinib.

Pages (from-to) 299-234
Journal Journal of Chemistry and Application
Volume 60B
Issue number 1B
Publication status Published - May-2022
ISBN 1859-4069