The Detosylation of Chiral 1,2-Bis(tosylamides)

J Org Chem. 2021 Jul 2;86(13):9163-9180. doi: 10.1021/acs.joc.1c00359. Epub 2021 Jun 21.

Abstract

The deprotection of chiral 1,2-bis(tosylamides) to their corresponding 1,2-diamines is mostly unsuccessful under standard conditions. In a new methodology, the use of Mg/MeOH with sufficient steric additions allows the facile synthesis of 1,2-diamines in 78-98% yields. These results are rationalized using density functional theory and the examination of inner and outer-sphere reduction mechanisms.