以碳化钙为固体炔源可切换合成2-亚甲基-3-氨基二氢吲哚和2-甲基-3-氨基吲哚
Switchable Synthesis of 2-Methylene-3-aminoindolines and 2-Methyl-3-aminoindoles Using Calcium Carbide as a Solid Alkyne Source.
作者信息
Wang Zhiqiang, Zhang Zeshuai, Li Zheng
机构信息
College of Chemistry and Chemical Engineering, Northwest Normal University, Lanzhou, Gansu 730070, P. R. China.
出版信息
Org Lett. 2022 Nov 4;24(43):8067-8071. doi: 10.1021/acs.orglett.2c03406. Epub 2022 Oct 26.
The one-pot three-component method for the switchable synthesis of 2-methylene-3-aminoindolines and 2-methyl-3-aminoindoles by reactions of -(2-formylaryl)sulfonamides, secondary amines, and calcium carbide is described. This protocol has the salient features of the use of an inexpensive, abundant, and easy-to-handle solid alkyne source, avoiding the use of flammable and explosive gaseous acetylene as an original alkyne source. In addition, a wide scope of substrates, satisfactory yield, and simple workup procedure are also advantages of this method.
描述了一种一锅三组分方法，通过-(2-甲酰基芳基)磺酰胺、仲胺和碳化钙的反应可切换合成2-亚甲基-3-氨基吲哚啉和2-甲基-3-氨基吲哚。该方法具有使用廉价、丰富且易于处理的固体炔烃源这一显著特点，避免了使用易燃、易爆的气态乙炔作为原始炔烃源。此外，底物范围广、产率令人满意以及后处理程序简单也是该方法的优点。
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