Alpha-site direct amination method of heterocyclic aromatic hydrocarbon compounds such as pyrrole and benzofuran

• Main Authors: LIAO LIHUA, LAN WEIQIAO
• Format: Patent
• Language: Chinese; English
• Published: 11.10.2022
• Subjects: APPARATUS THEREFOR; CHEMISTRY; GENERAL METHODS OF ORGANIC CHEMISTRY; HETEROCYCLIC COMPOUNDS; METALLURGY; ORGANIC CHEMISTRY

The invention discloses a method for direct amination of alpha-position of heterocyclic aromatic hydrocarbon compounds such as pyrrole and benzofuran. The structure of an alpha-position amination product is represented and confirmed by methods such as 1H NMR, 13C NMR, MS, X-ray and the like. Different substituted heterocyclic aromatic hydrocarbon compounds such as pyrrole or benzofuran and the like are fully reacted with quinone diimine series compounds in a proper organic solvent under the condition of room temperature by taking a trace amount of Lewis acid as a catalyst, so that alpha-position one-step amination of the heterocyclic aromatic hydrocarbon compounds such as pyrrole or benzofuran and the like is realized, and the one-step amination of the heterocyclic aromatic hydrocarbon compounds such as pyrrole or benzofuran and the like is realized. Finally, a series of alpha-site C-N bond coupled derivatives of heterocyclic aromatic hydrocarbon compounds such as pyrrole or benzofuran are generated. Compared