Department of Medicinal Chemistry, School of Pharmacy, Qingdao University, Qingdao 266021, China.
Department of Orthopedics, Qingdao Municipal Hospital, Qingdao, 266011, China.
Org Biomol Chem. 2022 Aug 17;20(32):6334-6338. doi: 10.1039/d2ob01206e.
With the aid of acetic acid, a 1,10-conjugate addition-mediated formal [3 + 3] cyclization of alkynyl indole imine methides formed from α-(6-indolyl) propargylic alcohols with 1,3-dicarbonyl compounds such as 4-hydroxycoumarins and cyclohexane-1,3-diones was developed, which provided robust access to a wide range of pyranocoumarin and pyran derivatives containing an indole skeleton with high efficiency under mild conditions.
在乙酸的辅助下,通过α-(6-吲哚基)炔丙醇与 1,3-二羰基化合物(如 4-羟基香豆素和环己烷-1,3-二酮)的 1,10-共轭加成介导的形式[3+3]环化反应,形成了炔基吲哚亚胺甲叉,为高效温和条件下合成含有吲哚骨架的广泛的吡喃香豆素和吡喃衍生物提供了一种强有力的方法。