METHOD FOR PREPARATION OF ERLOTINIB AND ITS PHARMACEUTICALLY ACCEPTABLE SALTS

Title:

METHOD FOR PREPARATION OF ERLOTINIB AND ITS PHARMACEUTICALLY ACCEPTABLE SALTS

Document Type and Number:

Japanese Patent JP2014129362

Kind Code:

A

Abstract:

PROBLEM TO BE SOLVED: To provide an improved method for the synthesis of erlotinib (N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine) and its pharmaceutically acceptable salts.SOLUTION: A method comprises reacting a 4-halo-6,7-bis(2-methoxyethoxy) quinazoline with 3-aminophenyl acetylene or a salt thereof under acidic conditions where an acid is used which may be selected from the group consisting of hydrochloric acid, hydrobromic acid, sulfuric acid, p-toluene sulfonic acid, benzoic acid, citric acid, succinic acid, oxalic acid, benzene sulfonic acid, tartaric acid, methane sulfonic acid, phosphoric acid and mixtures thereof, thereby forming the corresponding acid salt of erlotinib shown in formula described below.

Inventors:

DHARMARAJ RAMACHANDRA RAO
RAJENDRA NARAYANRAO KANKAN

Application Number:

JP2014018797A

Publication Date:

July 10, 2014

Filing Date:

February 03, 2014

Export Citation:

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Assignee:

CIPLA LTD

International Classes:

C07D239/94; A61K31/517; A61P43/00; C07B61/00

Domestic Patent References:

JPH10506633A	1998-06-30
JP2002513009A	2002-05-08

Other References:

Ｃ．Ｇ．ＷＥＲＭＵＴＨ編, 「最新　創薬化学　下巻」, vol. ３４７〜３６５頁, JPN6014029314, 1999, ISSN: 0002974777
TIMOTHY NORRIS, JOURNAL OF THE CHEMICAL SOCIETY, PERKIN TRANSACTIONS 2, vol. V12, JPN5010004112, 2000, pages 2498 - 2502, ISSN: 0002974778

Attorney, Agent or Firm:

Kurata Masatoshi
Yoshihiro Fukuhara
Nobuhisa Nogawa
Takashi Mine
Naoki Kono
Katsu Sunagawa
Morisezo Iseki
Tatsushi Sato
Takashi Okada
Mihoko Horiuchi

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