Articles

The Synthesis of Cancer Treatment Medicine Erlotinib

  • WANG Xian;SONG Fang;FENG Qingwei
Expand
  • 1. Chemistry Division of Patent Examination Cooperation Center, State Intellectual Property Office of the People's Republic of China, Beijing 100083, China;2. China Animal Husbandry Institute, Beijing 102206, China

Received date: 2011-08-31

  Revised date: 2012-01-15

  Online published: 2012-02-18

Abstract

The concise synthesis of Erlotinib was described. Treatment of Ethyl 3,4-dihydroxybenzoate with 2-methoxyethyl methanesulfonate followed by nitration, reduction, cyclization and chloration to afford 4-chloro-6,7-bis(2-methoxyethoxy)-1,4-dihydroquinazoline, which was treated with 3-ethynylaniline and then with dry hydrochloride to give Erlotinib. In this synthesis, the nitration process has greatly been improved. The advantages of this synthetic route include short reaction time, good total yield, and simple work-up.

Key words: Erlotinib; nitration; synthesis

Cite this article

WANG Xian;SONG Fang;FENG Qingwei . The Synthesis of Cancer Treatment Medicine Erlotinib[J]. Science & Technology Review, 2012 , 30(5) : 49 -51 . DOI: 10.3981/j.issn.1000-7857.2012.05.007

Outlines

/