Difunctionalization of Cyclopropyl Amines with N-lodosuccinirnide (NIS) or in Situ Formed Cyanogen Iodide (ICN)

by Wang, Qile; Zheng, Nan

We report herein a 1,3-difunctionalization of c-yclopropylamines thaf serve as 'a A- nucleophile in a two electron (2e) 5,2-like ring opening pathway. N-Iodosuccinimide (NIS) or in situ generated cyanogen iodide (ICN) is employed as electrophilic iodinating reagents in conjunction with TMSCN or succinimide to furnish multiple pairs of functional groups disposed in a 1,3 -manner. This 2e ring opening manifold overcomes the constraint of our previously reported le protocol as demonstrated by successful activation of monocyclic tertiary cyclopropylamines.

Journal
Organic Letters
Volume
21
Issue
24
Year
2019
Start Page
9999-10002
URL
https://dx.doi.org/10.1021/acs.orglett.9b03922
ISBN/ISSN
1523-7052; 1523-7060
DOI
10.1021/acs.orglett.9b03922