Department of Chemistry, Indian Institute of Technology Hyderabad, Kandi, Sangareddy 502285, Telangana, India.
Org Lett. 2021 Oct 1;23(19):7353-7358. doi: 10.1021/acs.orglett.1c02460. Epub 2021 Sep 14.
Herein, we present -C-H olefination on derivatives of phenylacetic acids by tethering with a simple nitrile-based template through palladium catalysis. Notably, the versatility of the method is evaluated with a wide range of phenylacetic acid derivatives for obtaining the -olefination products in fair to excellent yields with outstanding selectivities under mild conditions. Significantly, the present strategy is successfully exemplified for the synthesis of drugs/natural product analogues (naproxen, ibuprofen, paracetamol, and cholesterol).
在此，我们通过钯催化将简单的基于腈的模板与苯乙酸衍生物连接，展示了 -C-H 烯烃化反应。值得注意的是，该方法的多功能性通过广泛的苯乙酸衍生物进行了评估，以在温和条件下获得中等至优异收率的 -烯烃化产物，并具有出色的选择性。重要的是，本策略成功地应用于药物/天然产物类似物（萘普生、布洛芬、扑热息痛和胆固醇）的合成。
