使用 LiO-t-Bu/CsF 在 2-烷基杂芳烃中双羧化两个 C-H 键。
Double-Carboxylation of Two C-H Bonds in 2-Alkylheteroarenes Using LiO- t-Bu/CsF.
机构信息
Department of Biophysical Chemistry, Graduate School of Pharmaceutical Sciences , Tohoku University , Aoba, Sendai 980-8578 , Japan.
出版信息
Org Lett. 2019 Jun 21;21(12):4515-4519. doi: 10.1021/acs.orglett.9b01386. Epub 2019 May 31.
We describe the double-carboxylation of two C-H bonds (i.e., at the benzylic and the β-positions) in 2-alkylheteroarenes using a combination of LiO- t-Bu and CsF. A diverse range of substrates, namely benzothiophene, thiophene, benzofuran, furan, and indole derivatives, are efficiently converted into the doubly carboxylated products. A variety of functionalities (i.e., methyl, methoxy, halogen, cyano, ester, ketone, and amide moieties) are well tolerated.
我们描述了使用 LiO-t-Bu 和 CsF 的组合，在 2-烷基杂芳烃中双羧化两个 C-H 键（即在苄位和 β-位）。各种底物，即苯并噻吩、噻吩、苯并呋喃、呋喃和吲哚衍生物，被有效地转化为双羧化产物。多种官能团（即甲基、甲氧基、卤素、氰基、酯、酮和酰胺部分）具有良好的耐受性。
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