CuI 催化的 4-碘吡唑与醇的偶联反应：在 Withasomnine 和同系物合成中的应用。
CuI-Catalyzed Coupling Reactions of 4-Iodopyrazoles and Alcohols: Application toward Withasomnine and Homologs.
机构信息
Department of Pharmaceutical Organic Chemistry, Osaka University of Pharmaceutical Sciences, 4-20-1 Nasahara, Takatsuki, Osaka 569-1094, Japan.
出版信息
Molecules. 2021 Jun 2;26(11):3370. doi: 10.3390/molecules26113370.
The direct 4-alkoxylation of 4-iodo-1-pyrazoles with alcohols was achieved by a CuI-catalyzed coupling protocol. The optimal reaction conditions employed excess alcohol and potassium -butoxide (2 equiv) in the presence of CuI (20 mol%) and 3,4,7,8-tetramethyl-1,10-phenanthroline (20 mol%) at 130 °C for 1 h under microwave irradiation. The present method was efficiently applied to the synthesis of withasomnine and its six- and seven-membered cyclic homologs.
碘化 1-吡唑与醇的直接 4-烷氧基化反应是通过 CuI 催化偶联实现的。优化的反应条件是在 130°C 下微波辐射 1 小时，使用过量的醇和叔丁醇钾（2 当量），CuI（20mol%）和 3,4,7,8-四甲基-1,10-菲咯啉（20mol%）作为催化剂。本方法有效地应用于合成瓦他索宁及其六元和七元环同系物。
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