铜催化炔烃的三氟甲基化/环化反应合成二氧二苯并噻氮杂卓
Copper-Catalyzed Trifluoromethylation/Cyclization of Alkynes for Synthesis of Dioxodibenzothiazepines.
作者信息
Zhang Zi-Qi, Xu Yi-Hao, Dai Jing-Cheng, Li Yan, Sheng Jie, Wang Xi-Sheng
机构信息
Hefei National Laboratory for Physical Sciences at the Microscale and Department of Chemistry, University of Science and Technology of China, 96 Jinzhai Road, Hefei, Anhui 230026, China.
出版信息
Org Lett. 2021 Mar 19;23(6):2194-2198. doi: 10.1021/acs.orglett.1c00344. Epub 2021 Feb 26.
A facile and efficient approach for the synthesis of the CF-containing dioxodibenzothiazepines has been developed via copper-catalyzed trifluoromethylation/cyclization of alkynes utilizing a radical relay strategy. This method has demonstrated low catalyst loading, high regiocontrol, and broad scope under mild conditions. Good compatibility for the N-protecting group, gram-scale experiment, and further derivation of product prove the versatility of this transformation.
通过自由基接力策略，利用铜催化的炔烃三氟甲基化/环化反应，开发了一种简便高效的合成含CF二氧二苯并噻氮杂䓬的方法。该方法在温和条件下表现出低催化剂用量、高区域选择性和广泛的底物范围。对N-保护基具有良好的兼容性、克级规模实验以及产物的进一步衍生化证明了该转化反应的通用性。
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