Key Laboratory of Green Chemistry and Technology of Ministry of Education, College of Chemistry, Sichuan University , 29 Wangjiang Road, Chengdu 610064, China.
Org Lett. 2017 Sep 15;19(18):4830-4833. doi: 10.1021/acs.orglett.7b02265. Epub 2017 Aug 30.
β-Azolyl propanoic acid derivatives are frequently found in biologically active molecules and pharmaceuticals. Here, we report the oxidative heteroarylation of unactivated C(sp)-H bonds with azole C(sp)-H bonds via copper or nickel catalysis with the aid of removable bidentate auxiliary, which provides a rapid pathway to β-azolyl propanoic acid derivatives. A variety of azoles such as oxazole, benzoxazole, thiazole, benzothiazoles, benzimidazole, purine, and even [1,2,4]triazolo[1,5-a]pyrimidine could be engaged in this protocol.
β-唑基丙酸衍生物在生物活性分子和药物中经常被发现。在这里，我们报告了在铜或镍催化下，通过可去除的双齿辅助试剂，实现未活化的 C(sp)-H 键与唑 C(sp)-H 键的氧化杂芳基化反应，为β-唑基丙酸衍生物提供了一条快速途径。各种唑类，如恶唑、苯并恶唑、噻唑、苯并噻唑、苯并咪唑、嘌呤，甚至[1,2,4]三唑并[1,5-a]嘧啶，都可以参与这个反应。
