Route Design and Development of c-Met Inhibitor LY2801653

来源 :The 24th International Society of Heterocyclic Chemistry Con | 被引量 : 0次 | 上传用户:shahua001
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An overall 22% yield synthesis of a MET kinase inhibitor LY2801653 was achieved over eight steps, starting with 3-hydroxybenzaldehyde.Highlights of the process chemistry design and development include: a Cu-catalyzed cyclization to selectively form an N 1-methylindazole ring, a selective nitro reduction in the presence of an aryl bromide, a late stage Suzuki cross-coupling, and a base promoted Boc-deprotection to form the desired drug candidate.
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