A one-pot selective synthesis of N-Boc protected secondary amines: tandem direct reductive amination/N-Boc protection

作者：Neelarapu Raghupathi; Petukhov Pavel A^*

来源：Tetrahedron, 2012, 68(35): 7056-7062.

DOI：10.1016/j.tet.2012.06.055

• Direct reductive amination
• Secondary amines
• N-Boc protection
• Sodium triacetoxyborohydride
• Tandem reaction

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.

• 出版日期2012-9-2