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直接 C-H 烯丙基化 N-酰基/砜基四氢异喹啉及其类似物。

Direct C-H Allylation of N-Acyl/Sulfonyl Tetrahydroisoquinolines and Analogues.

机构信息

State Key Laboratory of Elemento-Organic Chemistry, Research Institute of Elemento-Organic Chemistry, Collaborative Innovation Center of Chemical Science and Engineering (Tianjin), Nankai University , Tianjin, 300071, People's Republic of China.

出版信息

Org Lett. 2015 Nov 20;17(22):5714-7. doi: 10.1021/acs.orglett.5b03042. Epub 2015 Nov 11.

Abstract

A highly efficient direct C-H allylation reaction at the α position of N-acyl/sulfonyl tetrahydroisoquinolines under mild conditions was developed. The reaction was also suitable for allylation of other protected nitrogen-containing heterocycles. Several interesting transformations of the products into valuable synthetic intermediates are featured with the successful total synthesis of (±)-crispine A.

摘要

发展了一种在温和条件下高效的直接 C-H 烯丙基化反应,该反应发生在 N-酰基/磺酰基四氢异喹啉的α 位。该反应也适用于其他保护的含氮杂环的烯丙基化。通过成功地全合成(±)-crispine A,展示了产物转化为有价值的合成中间体的几个有趣的转化。

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