Synthesis 2012; 44(15): 2469-2473
DOI: 10.1055/s-0032-1316550
paper
© Georg Thieme Verlag Stuttgart · New York

Reductive Amination by Continuous-Flow Hydrogenation: Direct and Scalable Synthesis of a Benzylpiperazine

Jing Liu*, Anne E. Fitzgerald, Neelakandha S. Mani
  • Janssen Research & Development, L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA, Fax: +1(858)3203354   Email: jliu30@its.jnj.com
Further Information

Publication History

Received: 19 March 2012

Accepted after revision: 18 May 2012

Publication Date:
02 July 2012 (eFirst)

Abstract

A benzylpiperazine was prepared directly from the corresponding benzaldehyde and piperazine on a continuous-flow hydrogenation apparatus. The synthesis was protecting group free, safe, and environmentally friendly. Large-scale synthesis under flow hydrogenation conditions was also demonstrated.

Supporting Information