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Continuous Amination of Aryl/Heteroaryl Halides Using Aqueous Ammonia in a Teflon AF-2400 Tube-in-Tube Micro-Flow Reactor

wu, jie and xue, chengwen and li, jiesheng and lee, jin ping (2019) Continuous Amination of Aryl/Heteroaryl Halides Using Aqueous Ammonia in a Teflon AF-2400 Tube-in-Tube Micro-Flow Reactor. Reaction Chemistry & Engineering, 4 (2). pp. 346-350. ISSN 2058-9883

Abstract

The annual production of primary (hetero)arylamines has exceeded 6 million tons and has been extensively employed in pharmaceutical, agrochemical, and material industries. Catalyst-free and protecting group free nucleophilic amination using ammonia represents a green and atom-economical method. However due to the innate reactivity, chemical compatibility issue and the safety hazardous property of ammonia gas, such transformation is still underused. By implementing the gas permeable Teflon AF-2400 tube-in-tube system, diffusion of NH3 from aqueous ammonia to reaction mixture for amination can be achieved in a continuous flow fashion. In this communication, we herein report the use of aqueous ammonia as NH3 source in amination of hetereoaryl chorides to generate primary heteroaryl amines, providing a protocol that is green, economical and safe.

Item Type: Article
Date Deposited: 27 Feb 2019 00:45
Last Modified: 27 Feb 2019 00:45
URI: https://oak.novartis.com/id/eprint/38365

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