The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Dec. 25, 2007

Filed:

Nov. 06, 2002
Applicants:

Arie Gutman, Haifa, IL;

Gennadi Nisnevich, Haifa, IL;

Lev Yudovitch, Haifa, IL;

Inventors:

Arie Gutman, Haifa, IL;

Gennadi Nisnevich, Haifa, IL;

Lev Yudovitch, Haifa, IL;

Assignee:

ISP Investments Inc., Wilmington, DE (US);

Attorney:
Primary Examiner:
Int. Cl.
CPC ...
C07D 307/81 (2006.01); C07D 307/83 (2006.01); C07C 233/25 (2006.01); C07C 271/28 (2006.01); C07C 271/58 (2006.01);
U.S. Cl.
CPC ...
Abstract

The present invention provides, according to an aspect thereof, a novel process for the preparation of dronedarone [1] and pharmaceutically acceptable salts thereof. According to a preferred embodiment, the process comprises N-acetylating of p-anisidine or p-phenetidine with acetic anhydride, reacting of the obtained N-(4-alkoxyphenyl)acetamide with 2-bromohexanoyl chloride or bromide in the presence of aluminum chloride or bromide to obtain N-[3-(2-bromohexanoyl)-4-hydroxyphenyl]acetamide [6], converting the compound [6] into 2-butyl-5-benzofuranamine hydrochloride [12] and subsequently converting [12] into [1] or pharmaceutically acceptable salts thereof. In accordance with another aspect of this invention, there are provided novel intermediates, inter alia the novel compounds [6] and [12]. The novel intermediates of the present invention are stable, solid compounds, obtainable in high yields, which can be easily purified by crystallization and stored for long periods of time.


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