Vertex Pharmaceuticals Incorporated, Department of Chemistry 11010 Torreyana Road, San Diego, California 92121, United States.
Org Lett. 2015 May 15;17(10):2362-5. doi: 10.1021/acs.orglett.5b00861. Epub 2015 Apr 27.
A radical mediated C-H functionalization of 3,6-dichloropyridazine using primary alcohols, t-BuOOH, and TiCl3 to access alkoxy pyridazines is described. This transformation is conducted open to air and on gram scale. A subsequent cyclization step can then be employed to efficiently access diversely substituted tetrahydropyridopyridazines with multiple functional handles.
本文描述了一种使用伯醇、t-BuOOH 和 TiCl3 介导的 3,6-二氯哒嗪的 C-H 功能化反应，从而构建烷氧基哒嗪。该转化在开放体系和克级规模下进行。随后可以进行环化步骤，有效地构建具有多个功能基团的多取代四氢吡啶并哒嗪。
