A Different Approach to the EGFR Inhibitor Gefitinib Involving Solid-Phase Synthesis

Author:

Carvalho Luísa1ORCID,Sequeira André1,Lourenço Ana1,Ferreira Luísa1,Branco Paula1,Mendes Zita2,Lourenço Nuno2,Figueiredo Margarida2

Affiliation:

1. LAQV, REQUIMTE, Departamento de Química, Faculdade de Ciências e Tecnologia, Universidade NOVA de Lisboa

2. Hovione FarmaCiencia SA, R&D, Campus do Lumiar

Abstract

An efficient solid-phase synthesis approach is here reported for the first time to prepare the EGFR inhibitor Gefitinib. The five-step synthetic strategy used FMP resin as the solid support, and FTIR and colorimetric assays were used to track the reaction’s progress. Gefitinib was obtained with an overall yield of 40%.

Funder

Ministério da Educação e Ciência

Publisher

Georg Thieme Verlag KG

Subject

Organic Chemistry

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