Bcworld Pharm. Co., Ltd.

Jong Sun Lee

Seung Ki Kim

Hearan Suh

Sang Kyu Nam

A method for preparing an imatinib base includes reacting 4-(4-methyl-piperazinomethyl)-benzoic acid with a 2,2'-dibenzothiazolyl disulfide derivative in the presence of a phosphine derivative to prepare a novel thioester compound and preparing an imatinib base using the thioester compound as a reaction intermediate. With the method, imatinib base in higher yield and/or purity can be prepared cost-effectively.

Method for producing imatinib base

The present invention relates to a novel method for preparing an imatinib base, and more particularly to a method for preparing an imatinib base, which comprises reacting 4-(4-methyl-piperazinomethyl)-benzoic acid with a 2,2'-dibenzothiazolyl disulfide derivative in the presence of a phosphine derivative to prepare a novel thioester compound and preparing an imatinib base using the thioester compound as a reaction intermediate. In addition, the invention provides a novel thioester compound, which is used in the preparation of imatinib base, and a preparation method thereof. Ultimately, the invention provides a method of preparing the imatinib base in an economic manner and in high yield and purity and is expected to be used in the commercial production of large amounts of the imatinib base.

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Gyeonddi-do, South Korea

Jong Sun Lee