A one-pot selective synthesis of N-Boc protected secondary amines: tandem direct reductive amination/N-Boc protection
作者:Raghupathi Neelarapu、Pavel A. Petukhov
DOI:10.1016/j.tet.2012.06.055
日期:2012.9
A one-pot tandem direct reductive amination of aldehydes with primary amines resulting in N-Boc secondary amines using a (Boc)(2)O/sodium triacetoxyborohydride (STAB) system is reported. The tandem procedure is efficient, selective, and versatile, giving excellent yields of N-Boc protected secondary amines even in those cases where the products are prone to intramolecular lactamization. (C) 2012 Elsevier Ltd. All rights reserved.