Wang Zhiqiang, Zhang Zeshuai, Li Zheng
College of Chemistry and Chemical Engineering, Northwest Normal University, Lanzhou, Gansu 730070, P. R. China.
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。
