Direct oxidative C-H alkynylation of N-carbamoyl tetrahydroisoquinolines and dihydroisoquinolines.
Direct oxidative C-H alkynylation of N-carbamoyl tetrahydroisoquinolines and dihydroisoquinolines.
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DOI：
10.1039/c8ob00373d
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发表时间：
2018-04
影响因子：
3.2
通讯作者：
Lei Chen;Chuanxi Sun;Guidong Feng;Minyi Cao;Shuiai Zhao;Jun Yan;Ren-zhong Wan;Lei Liu
中科院分区：
文献类型：
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作者：
Lei Chen;Chuanxi Sun;Guidong Feng;Minyi Cao;Shuiai Zhao;Jun Yan;Ren-zhong Wan;Lei Liu
建立了TEMPO氧铵盐介导的n -氨基甲酰基四氢异喹啉类化合物的高效C-H烷基化反应。多种电子变化的n -氨基甲酰四氢异喹啉在温和的无金属条件下与一系列炔基三氟硼酸钾顺利反应。二氢异喹啉也是反应的合适组分。进一步证明了该方法易于获得结构多样的生物活性分子的合成适用性。
An efficient oxidative C-H alkynylation of N-carbamoyl tetrahydroisoquinolines mediated by a TEMPO oxoammonium salt has been established. A variety of electronically varied N-carbamoyl tetrahydroisoquinolines reacted with a range of alkynyl potassium trifluoroborates smoothly under mild metal-free conditions. Dihydroisoquinolines were also suitable components for the reaction. The synthetic applicability of the method for facile access to structurally diverse bioactive molecules was further demonstrated.