醚和 TMSI 通过 Catellani 策略实现芳基碘的 C-H 羟烷基化或甲基化。
C-H Hydroxyalkylation or Methylation of Aryl Iodides by Ethers and TMSI via a Catellani Strategy.
机构信息
State Key Laboratory of Applied Organic Chemistry, Lanzhou University, Lanzhou 730000, China.
College of Chemistry and Chemical Engineering, Northwest Normal University, Lanzhou 730070, China.
出版信息
Org Lett. 2022 Sep 30;24(38):6897-6902. doi: 10.1021/acs.orglett.2c02425. Epub 2022 Sep 16.
In this paper, in the presence of trimethylsilyl iodide, the direct -C-H hydroxyalkylation/methylation of aryl iodines was effectively realized via palladium/norbornene cooperative catalysis when low-cost tetrahydrofuran and 1,2-dimethoxyethane were used as alkyl sources. Heck, Suzuki, and Sonogashira coupling and hydrogenation were all compatible with the reaction as termination steps. In addition, neuromuscular agents and cardiovascular agents were synthesized in one step by this method, showing their potential application value.
本文在碘化三甲基硅烷的存在下，通过钯/降冰片烯协同催化，有效地实现了廉价的四氢呋喃和 1,2-二甲氧基乙烷作为烷基源时芳基碘的直接-C-H 羟烷基化/甲基化反应。Heck、Suzuki 和 Sonogashira 偶联以及氢化都是相容的反应终止步骤。此外，该方法还一步合成了神经肌肉药物和心血管药物，显示出其潜在的应用价值。
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