4.5 Article

One-Pot Three-Component Synthesis of 2-Methyl-3-aminobenzofurans Using Calcium Carbide as a Concise Solid Alkyne Source

Journal

CHINESE JOURNAL OF CHEMISTRY
Volume 39, Issue 11, Pages 2990-2994

Publisher

WILEY-V C H VERLAG GMBH
DOI: 10.1002/cjoc.202100383

Keywords

Cyclization; Multicomponent reactions; Synthetic methods; Calcium carbide; Alkyne source; Benzofuran

Funding

  1. National Natural Science Foundation of China [21462038]
  2. Key Laboratory of Eco-Environment-Related Polymer Materials of the Ministry of Education of China

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The method utilizes calcium carbide as a solid alkyne source to efficiently synthesize 2-methyl-3-aminobenzofurans, avoiding the use of flammable and explosive acetylene gas. It offers the advantages of being cost-effective, abundant, and easy to handle.
Main observation and conclusion A one-pot three-component method for the synthesis of 2-methyl-3-aminobenzofurans using calcium carbide as a concise solid alkyne source, and salicylaldehydes and secondary amines as starting materials is described. This protocol has salient feature of the use of inexpensive, abundant and easy-to-handle alkyne source, avoiding the use of inflammable and explosive acetylene gas as an original alkyne source. In addition, step economy, satisfactory yield, and simple work-up procedure are also advantages of this route.

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